Target Information

Target General Information

Target ID

T11764 (Former ID: TTDNR00661)

Target Name

Discoidin domain-containing receptor 2 (DDR2)

Synonyms

Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B

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Gene Name

DDR2

Target Type

Patented-recorded target

[1]

Function

Tyrosine kinase that functions as cell surface receptor for fibrillar collagen and regulates cell differentiation, remodeling of the extracellular matrix, cell migration and cell proliferation. Required for normal bone development. Regulates osteoblast differentiation and chondrocyte maturation via a signaling pathway that involves MAP kinases and leads to the activation of the transcription factor RUNX2. Regulates remodeling of the extracellular matrix by up-regulation of the collagenases MMP1, MMP2 and MMP13, and thereby facilitates cell migration and tumor cell invasion. Promotes fibroblast migration and proliferation, and thereby contributes to cutaneous wound healing.

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BioChemical Class

Kinase

UniProt ID

DDR2_HUMAN

EC Number

EC 2.7.10.1

Sequence

MILIPRMLLVLFLLLPILSSAKAQVNPAICRYPLGMSGGQIPDEDITASSQWSESTAAKY
GRLDSEEGDGAWCPEIPVEPDDLKEFLQIDLHTLHFITLVGTQGRHAGGHGIEFAPMYKI
NYSRDGTRWISWRNRHGKQVLDGNSNPYDIFLKDLEPPIVARFVRFIPVTDHSMNVCMRV
ELYGCVWLDGLVSYNAPAGQQFVLPGGSIIYLNDSVYDGAVGYSMTEGLGQLTDGVSGLD
DFTQTHEYHVWPGYDYVGWRNESATNGYIEIMFEFDRIRNFTTMKVHCNNMFAKGVKIFK
EVQCYFRSEASEWEPNAISFPLVLDDVNPSARFVTVPLHHRMASAIKCQYHFADTWMMFS
EITFQSDAAMYNNSEALPTSPMAPTTYDPMLKVDDSNTRILIGCLVAIIFILLAIIVIIL
WRQFWQKMLEKASRRMLDDEMTVSLSLPSDSSMFNNNRSSSPSEQGSNSTYDRIFPLRPD
YQEPSRLIRKLPEFAPGEEESGCSGVVKPVQPSGPEGVPHYAEADIVNLQGVTGGNTYSV
PAVTMDLLSGKDVAVEEFPRKLLTFKEKLGEGQFGEVHLCEVEGMEKFKDKDFALDVSAN
QPVLVAVKMLRADANKNARNDFLKEIKIMSRLKDPNIIHLLAVCITDDPLCMITEYMENG
DLNQFLSRHEPPNSSSSDVRTVSYTNLKFMATQIASGMKYLSSLNFVHRDLATRNCLVGK
NYTIKIADFGMSRNLYSGDYYRIQGRAVLPIRWMSWESILLGKFTTASDVWAFGVTLWET
FTFCQEQPYSQLSDEQVIENTGEFFRDQGRQTYLPQPAICPDSVYKLMLSCWRRDTKNRP
SFQEIHLLLLQQGDE

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3D Structure

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AlphaFold

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

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Ligand Name: 2-[4,5-bis(fluoranyl)-2-oxidanylidene-1'-(1~{H}-pyrazolo[3,4-b]pyridin-5-ylcarbonyl)spiro[indole-3,4'-piperidine]-1-yl]-~{N}-[2,2,2-tris(fluoranyl)ethyl]ethanamide

Ligand Info

Structure Description

Crystal Structure of human DDR2 kinase in complex with 2-[4,5-difluoro-2-oxo-1'-(1H-pyrazolo[3,4-b]pyridine-5-carbonyl)spiro[indole-3,4'-piperidine]-1-yl]-N-(2,2,2-trifluoroethyl)acetamide

PDB:6FER

Method

X-ray diffraction

Resolution

2.87 Å

Mutation

[3]

PDB Sequence

VAVEEFPRKL

⁶⁰⁹

LTFKEKLGEG

⁶¹⁹

QFGEVHLCEV

⁶²⁹

EGPVLVAVKM

⁶⁵⁶

LRADANKNAR

⁶⁶⁶

NDFLKEIKIM

⁶⁷⁶

SRLKDPNIIH

⁶⁸⁶

LLAVCITDDP

⁶⁹⁶

LCMITEYMEN

⁷⁰⁶

GDLNQFLSRH

⁷¹⁶

TVSYTNLKFM

⁷³⁷

ATQIASGMKY

⁷⁴⁷

LSSLNFVHRD

⁷⁵⁷

LATRNCLVGK

⁷⁶⁷

NYTIKIADFG

⁷⁷⁷

MSRNLYSGDY

⁷⁸⁷

YRIQGRAVLP

⁷⁹⁷

IRWMSWESIL

⁸⁰⁷

LGKFTTASDV

⁸¹⁷

WAFGVTLWET

⁸²⁷

FTFCQEQPYS

⁸³⁷

QLSDEQVIEN

⁸⁴⁷

TGEFFRDQGR

⁸⁵⁷

QTYLPQPAIC

⁸⁶⁷

PDSVYKLMLS

⁸⁷⁷

CWRRDTKNRP

⁸⁸⁷

SFQEIHLLLL

⁸⁹⁷

Residue

Distance (Å)

LEU616

3.753

VAL624

3.075

ALA653

3.515

LYS655

3.797

GLU672

3.643

MET676

3.373

LEU679

3.796

ILE684

3.668

ILE685

3.296

LEU687

4.473

MET699

3.327

ILE700

3.798

THR701

3.017

Residue

Distance (Å)

GLU702

4.127

TYR703

3.092

MET704

3.019

GLY707

4.876

LEU748

4.188

PHE753

3.408

HIS755

3.541

LEU764

3.497

ILE773

3.829

ALA774

2.795

ASP775

2.650

PHE776

3.130

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Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues. The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021). Human Similarity Proteins Human Tissue Distribution

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.

The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021).

Human Similarity Proteins

Human Tissue Distribution

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Mixed lineage kinase 1 (MAP3K9)	PF00069 ; PF14604	31.544 (94/298)	2.53E-28
Omphalocele kinase 1 (NUAK1)	PF00069	31.651 (69/218)	6.91E-17
Cyclin-dependent kinase 2 (CDK2)	PF00069	26.460 (77/291)	1.70E-16
Fused homolog (STK36)	PF13646 ; PF00069	29.767 (64/215)	1.97E-16
Cyclin-dependent kinase 3 (CDK3)	PF00069	28.767 (63/219)	3.93E-16
Cyclin-dependent kinase-like 2 (CDKL2)	PF00069	27.397 (60/219)	6.68E-16
Cyclin-dependent kinase 1 (CDK1)	PF00069	29.091 (64/220)	8.42E-16
Cyclin-dependent kinase 17 (CDK17)	PF12330 ; PF00069	25.632 (71/277)	1.84E-15
Cyclin-dependent kinase 13 (CDK13)	PF12330 ; PF00069	29.796 (73/245)	3.09E-15
Cyclin-dependent kinase 12 (CDK12)	PF00069	29.870 (69/231)	3.15E-15
NUAK family SNF1-like kinase 2 (NUAK2)	PF00069	30.493 (68/223)	3.63E-15
Cyclin-dependent kinase-like 4 (CDKL4)	PF00069	26.728 (58/217)	8.90E-15
Serine/threonine-protein kinase 33 (STK33)	PF00069	26.459 (68/257)	1.22E-14
Cyclin-dependent kinase 16 (CDK16)	PF12330 ; PF00069	26.339 (59/224)	1.32E-14
NIMA-related kinase 7 (NEK7)	PF00069	26.267 (57/217)	1.48E-14
Cyclin-dependent kinase 18 (CDK18)	PF00069	25.725 (71/276)	2.59E-14
Serine/threonine-protein kinase 24 (STK24)	PF00069	26.908 (67/249)	3.56E-14
Serine/threonine-protein kinase Nek11 (NEK11)	PF00069	25.974 (60/231)	3.91E-14
Oxidative stress responsive 1 (OXSR1)	PF12202 ; PF00069	23.019 (61/265)	4.19E-14
TAO kinase 1 (TAOK1)	PF00069	27.778 (65/234)	5.21E-14
NIMA-related kinase 6 (NEK6)	PF00069	25.651 (69/269)	6.08E-14
PKC-delta-interacting protein kinase (RIPK4)	PF12796 ; PF00069	26.778 (64/239)	6.83E-14
Cyclin-dependent kinase-like 1 (CDKL1)	PF00069	26.606 (58/218)	9.64E-14
Cyclin-dependent kinase 15 (CDK15)	PF00069	26.522 (61/230)	1.15E-13
Cyclin-dependent kinase 6 (CDK6)	PF00069	26.786 (60/224)	1.30E-13
Cyclin-dependent kinase 14 (CDK14)	PF00069	26.697 (59/221)	1.31E-13
cAMP-dependent protein kinase catalytic subunit beta (PRKACB)	PF00069	25.974 (60/231)	1.61E-13
Cyclin-dependent kinase 7 (CDK7)	PF00069	28.409 (75/264)	1.88E-13
Serine/threonine-protein kinase TAO2 (TAOK2)	PF00069	26.222 (59/225)	1.94E-13
Cyclin-dependent kinase 5 (CDK5)	PF00069	27.778 (60/216)	2.49E-13
Serine/threonine-protein kinase ULK1 (ULK1)	PF12063 ; PF00069	27.273 (51/187)	2.60E-13
RAC-gamma serine/threonine-protein kinase (AKT3)	PF00169 ; PF00069 ; PF00433 More >>	26.840 (62/231)	2.79E-13
Cyclin-dependent kinase 4 (CDK4)	PF00069	27.869 (51/183)	3.70E-13
Ste-20-related kinase (STK39)	PF12202 ; PF00069	23.985 (65/271)	4.69E-13
ERK activator kinase 5 (MAP2K5)	PF00564 ; PF00069	22.647 (77/340)	5.79E-13
Polo-like kinase 4 (PLK4)	PF00069 ; PF18190 ; PF18409 More >>	27.570 (59/214)	1.05E-12
Extracellular signal-regulated kinase 5 (ERK5)	PF00069	27.692 (54/195)	1.38E-12
RAC-beta serine/threonine-protein kinase (AKT2)	PF00169 ; PF00069 ; PF00433 More >>	24.893 (58/233)	1.39E-12
Inhibitor of nuclear factor kappa-B kinase alpha (IKKA)	PF18397 ; PF12179 ; PF00069 More >>	24.275 (67/276)	1.51E-12
Serine/threonine-protein kinase PAK 6 (PAK6)	PF00786 ; PF00069	24.377 (88/361)	1.91E-12
Serine/threonine-protein kinase ICK (CILK1)	PF00069	27.027 (60/222)	2.15E-12
Receptor-interacting serine/threonine-protein kinase 3 (RIPK3)	PF00069 ; PF12721	25.490 (78/306)	2.18E-12
PAK-2 protein kinase (PAK2)	PF00786 ; PF00069	23.077 (51/221)	2.29E-12
Protein kinase C delta (PRKCD)	PF00130 ; PF00069 ; PF00433 More >>	24.790 (59/238)	2.34E-12
Calmodulin-dependent kinase II (CAMKK2)	PF00069	33.140 (57/172)	2.54E-12
Unc-51 like kinase 3 (ULK3)	PF04212 ; PF00069	23.843 (67/281)	2.54E-12
Salt-inducible kinase 2 (SIK2)	PF00069	31.579 (54/171)	2.57E-12
Ribosomal protein S6 kinase alpha-2 (RSK2)	PF00069 ; PF00433	28.636 (63/220)	3.17E-12
SPS1/STE20-related protein kinase YSK4 (YSK4)	PF00069	24.648 (70/284)	4.44E-12
Doublecortin-like kinase 1 (DCLK1)	PF03607 ; PF00069	25.000 (59/236)	4.77E-12
PAK-1 protein kinase (PAK1)	PF00786 ; PF00069	23.377 (54/231)	5.13E-12
Protein kinase C theta (PRKCQ)	PF00130 ; PF00069 ; PF00433 More >>	24.681 (58/235)	5.64E-12
Serine/threonine-protein kinase PAK 3 (PAK3)	PF00786 ; PF00069	23.077 (51/221)	5.84E-12
Serine/threonine-protein kinase ULK2 (ULK2)	PF12063 ; PF00069	26.344 (49/186)	6.60E-12
Serine/threonine-protein kinase Nek8 (NEK8)	PF00069 ; PF00415	27.230 (58/213)	7.58E-12
Serine/threonine-protein kinase MARK2 (MARK2)	PF02149 ; PF00069 ; PF00627 More >>	27.344 (70/256)	7.60E-12
MAPK/ERK kinase kinase 1 (MAP3K1)	PF00069	23.810 (65/273)	8.03E-12
RAC-alpha serine/threonine-protein kinase (AKT1)	PF00169 ; PF00069 ; PF00433 More >>	27.155 (63/232)	8.76E-12
Cyclin-dependent kinase-like 5 (CDKL5)	PF00069	25.688 (56/218)	9.32E-12
SNF-related serine/threonine-protein kinase (SNRK)	PF00069	26.122 (64/245)	1.07E-11
G protein-coupled receptor kinase 6 (GRK6)	PF00069 ; PF00615	24.579 (73/297)	1.11E-11
Putative 3-phosphoinositide-dependent protein kinase 2 (PDPK2P)	PF00069	23.041 (50/217)	1.14E-11
G protein-coupled receptor kinase 5 (GRK5)	PF00069 ; PF00615	24.648 (70/284)	1.46E-11
Ribosomal protein S6 kinase alpha-3 (RSK3)	PF00069 ; PF00433	28.111 (61/217)	1.49E-11
Phosphoinositide dependent protein kinase-1 (PDPK1)	PF14593 ; PF00069	23.041 (50/217)	1.56E-11
Cyclin-dependent kinase-like 3 (CDKL3)	PF00069	23.853 (52/218)	1.91E-11
MAP/microtubule affinity-regulating kinase 4 (MARK4)	PF02149 ; PF00069 ; PF00627 More >>	32.353 (44/136)	1.96E-11
Serine/threonine-protein kinase 25 (STK25)	PF00069	22.680 (66/291)	2.25E-11
Calcium/calmodulin-dependent protein kinase type 1 (CAMK1)	PF00069	25.000 (63/252)	2.33E-11
Serine/threonine-protein kinase 17B (STK17B)	PF00069	22.789 (67/294)	2.74E-11
Calcium/calmodulin-dependent protein kinase type 1D (CAMK1D)	PF00069	25.397 (64/252)	2.79E-11
Aurora kinase A (AURKA)	PF00069	27.014 (57/211)	2.88E-11
cAMP-dependent protein kinase catalytic subunit alpha (PRKACA)	PF00069	26.168 (56/214)	2.90E-11
Mitogen-activated protein kinase 4 (MAPK4)	PF00069	30.769 (60/195)	3.12E-11
MEK kinase kinase 2 (MAP4K2)	PF00780 ; PF00069	23.605 (55/233)	3.81E-11
Microtubule affinity regulating kinase 3 (MARK3)	PF02149 ; PF00069 ; PF00627 More >>	29.480 (51/173)	4.07E-11
IL-1 receptor-associated kinase 1 (IRAK1)	PF00531 ; PF00069	23.967 (58/242)	4.15E-11
Inhibitor of nuclear factor kappa-B kinase beta (IKKB)	PF18397 ; PF12179 ; PF00069 More >>	26.316 (60/228)	4.26E-11
Calcium/calmodulin-dependent protein kinase type 1B (PNCK)	PF00069	26.800 (67/250)	4.38E-11
Serine/threonine-protein kinase MARK1 (MARK1)	PF02149 ; PF00069 ; PF00627 More >>	27.523 (60/218)	4.52E-11
MST-1 protein kinase (STK4)	PF11629 ; PF00069	23.529 (52/221)	5.09E-11
Salt-inducible kinase 1 (SIK1)	PF00069	32.353 (44/136)	5.15E-11
Putative serine/threonine-protein kinase SIK1B (SIK1B)	PF00069	32.353 (44/136)	5.15E-11
Serine/threonine-protein kinase MAK (MAK)	PF00069	25.664 (58/226)	5.17E-11
Leucine-rich repeat serine/threonine-protein kinase 1 (LRRK1)	PF12796 ; PF16095 ; PF00069 ; PF08477 More >>	26.056 (74/284)	5.77E-11
Protein kinase C beta (PRKCB)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	26.446 (64/242)	5.98E-11
ERK activator kinase 2 (MEK2)	PF00069	22.472 (40/178)	6.88E-11
Serine/threonine-protein kinase 26 (STK26)	PF00069	25.792 (57/221)	7.41E-11
Cyclin-dependent kinase 10 (CDK10)	PF00069	25.379 (67/264)	7.51E-11
Microtubule-associated serine/threonine-protein kinase 3 (MAST3)	PF08926 ; PF17820 ; PF02163 ; PF00069 More >>	27.473 (50/182)	9.51E-11
ERK activator kinase 1 (MEK1)	PF00069	23.034 (41/178)	9.66E-11
5'-AMP-activated protein kinase catalytic subunit alpha-2 (PRKAA2)	PF16579 ; PF00069	24.382 (69/283)	9.74E-11
cAMP-dependent protein kinase catalytic subunit gamma (PRKACG)	PF00069	25.701 (55/214)	1.32E-10
G protein-coupled receptor kinase 4 (GRK4)	PF00069 ; PF00615	24.380 (59/242)	1.42E-10
Titin (TTN)		26.360 (63/239)	1.43E-10
Hormonally up-regulated neu tumor-associated kinase (HUNK)	PF00069	23.214 (52/224)	1.77E-10
Ribosomal protein S6 kinase alpha-1 (RSK1)	PF00069 ; PF00433	25.338 (75/296)	1.99E-10
Putative serine/threonine-protein kinase PRKY (PRKY)	PF00069	25.778 (58/225)	2.12E-10
MAPK/ERK kinase kinase 3 (MAP3K3)	PF00564 ; PF00069	27.854 (61/219)	2.20E-10
NIMA-related kinase 1 (NEK1)	PF00069	22.831 (50/219)	2.24E-10
Aurora kinase C (AURKC)	PF00069	23.529 (64/272)	3.08E-10
cAMP-dependent protein kinase catalytic subunit PRKX (PRKX)	PF00069	26.222 (59/225)	3.47E-10
Serine/threonine-protein kinase WNK4 (WNK4)	PF12202 ; PF00069	24.415 (73/299)	3.75E-10
Death-associated protein kinase 1 (DAPK1)	PF00023 ; PF12796 ; PF13637 ; PF00531 ; PF00069 More >>	21.908 (62/283)	3.78E-10
Serine/threonine-protein kinase Nek5 (NEK5)	PF00069	23.926 (39/163)	4.18E-10
Serine/threonine-protein kinase tousled-like 2 (TLK2)	PF00069	23.293 (58/249)	4.41E-10
MAP kinase p38 (MAPK12)	PF00069	24.699 (41/166)	4.50E-10
Protein kinase C alpha (PRKCA)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	26.168 (56/214)	4.82E-10
TGF-beta receptor type I (TGFBR1)	PF01064 ; PF00069 ; PF08515 More >>	25.816 (87/337)	5.08E-10
Serine/threonine-protein kinase 3 (STK3)	PF11629 ; PF00069	23.849 (57/239)	5.27E-10
Myosin light chain kinase 2 (MYLK2)	PF00069	23.853 (52/218)	5.57E-10
Death-associated protein kinase 3 (DAPK3)	PF00069	25.279 (68/269)	5.80E-10
Rhodopsin kinase GRK1 (GRK1)	PF00069 ; PF00615	24.171 (51/211)	5.86E-10
Microtubule-associated serine/threonine-protein kinase 2 (MAST2)	PF08926 ; PF17820 ; PF00069 More >>	27.168 (47/173)	5.88E-10
Serine/threonine-protein kinase Nek3 (NEK3)	PF00069	23.214 (52/224)	6.08E-10
SIK family kinase 3 (SIK3)	PF00069	27.473 (50/182)	6.45E-10
STE20-related serine/threonine-protein kinase (SLK)	PF00069 ; PF12474	25.214 (59/234)	6.56E-10
PAS domain-containing serine/threonine-protein kinase (PASK)	PF13426 ; PF00069	26.255 (68/259)	7.39E-10
Calcium/calmodulin-dependent protein kinase type 1G (CAMK1G)	PF00069	24.000 (60/250)	7.87E-10
Stress-activated protein kinase 2b (p38 beta)	PF00069	24.786 (58/234)	8.04E-10
Serine/threonine-protein kinase NIM1 (NIM1K)	PF00069	26.705 (47/176)	8.31E-10
TAO kinase 3 (TAOK3)	PF00069	23.950 (57/238)	1.05E-09
Microtubule-associated serine/threonine-protein kinase 1 (MAST1)	PF08926 ; PF17820 ; PF00069 More >>	26.590 (46/173)	1.08E-09
Microtubule-associated serine/threonine-protein kinase 4 (MAST4)	PF08926 ; PF17820 ; PF02163 ; PF00069 More >>	27.168 (47/173)	1.08E-09
MEK kinase kinase 1 (MAP4K1)	PF00780 ; PF00069	24.107 (54/224)	1.13E-09
Doublecortin-like kinase 2 (DCLK2)	PF03607 ; PF00069	25.229 (55/218)	1.25E-09
Death-associated protein kinase 2 (DAPK2)	PF00069	22.968 (65/283)	1.29E-09
MAPK/ERK kinase kinase 4 (MAP3K4)	PF19431 ; PF00069	24.576 (58/236)	1.35E-09
Extracellular signal-regulated kinase 2 (ERK2)	PF00069	26.344 (49/186)	1.40E-09
Mitogen-activated protein kinase 15 (MAPK15)	PF00069	27.434 (62/226)	1.45E-09
Stress-activated protein kinase 2a (p38 alpha)	PF00069	24.096 (40/166)	1.47E-09
5'-AMP-activated protein kinase catalytic subunit alpha-1 (PRKAA1)	PF16579 ; PF00069	24.537 (53/216)	1.53E-09
Myosin light chain kinase 3 (MYLK3)	PF00069	24.658 (54/219)	1.95E-09
Mitogen-activated protein kinase 6 (MAPK6)	PF00069	28.333 (51/180)	2.46E-09
Serine/threonine-protein kinase PAK 5 (PAK5)	PF00786 ; PF00069	25.333 (57/225)	2.68E-09
Extracellular signal-regulated kinase 1 (ERK1)	PF00069	24.457 (45/184)	3.00E-09
Serine/threonine-protein kinase Sgk1 (SGK1)	PF00069 ; PF00433	25.581 (55/215)	3.23E-09
MAPK/ERK kinase kinase 2 (MAP3K2)	PF00564 ; PF00069	25.561 (57/223)	3.30E-09
Testis-specific serine kinase 2 (TSSK2)	PF00069	24.895 (59/237)	3.34E-09
Serine/threonine-protein kinase 10 (STK10)	PF00069 ; PF12474	24.167 (58/240)	3.44E-09
Cyclin-dependent kinase 11A (CDK11A)	PF00069	25.668 (48/187)	3.80E-09
Serine/threonine-protein kinase NLK (NLK)	PF00069	27.072 (49/181)	4.04E-09
CaM-kinase IV kinase (CAMKK1)	PF00069	29.091 (48/165)	4.22E-09
Cyclin-dependent kinase 20 (CDK20)	PF00069	27.108 (45/166)	4.61E-09
Serine/threonine-protein kinase H1 (PSKH1)	PF00069	24.294 (43/177)	4.98E-09
Cytoplasmic DRAK1 (STK17A)	PF00069	24.887 (55/221)	5.01E-09
Serine/threonine-protein kinase H2 (PSKH2)	PF00069	23.581 (54/229)	5.26E-09
Serine/threonine-protein kinase SBK1 (SBK1)	PF00069	25.095 (66/263)	5.43E-09
Serine/threonine-protein kinase Nek4 (NEK4)	PF00069	24.074 (52/216)	5.79E-09
Ribosomal protein S6 kinase alpha-6 (RSK6)	PF00069 ; PF00433	24.916 (74/297)	5.84E-09
Cyclin-dependent kinase 19 (CDK19)	PF00069	27.979 (54/193)	6.30E-09
PDZ binding kinase (PBK)	PF00069	27.757 (73/263)	6.91E-09
Testis-specific serine/threonine-protein kinase 4 (TSSK4)	PF00069	27.219 (46/169)	7.70E-09
Cyclin-dependent kinase 8 (CDK8)	PF00069	27.979 (54/193)	7.86E-09
Activin receptor type IB (ACVR1B)	PF01064 ; PF00069 ; PF08515 More >>	24.702 (83/336)	9.10E-09
Leucine-rich repeat kinase 2 (LRRK2)	PF16095 ; PF12799 ; PF13855 ; PF00069 ; PF08477 More >>	23.344 (74/317)	9.49E-09
MEK kinase kinase 3 (MAP4K3)	PF00780 ; PF00069	23.348 (53/227)	1.01E-08
Mitogen-activated protein kinase kinase kinase 15 (MAP3K15)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	25.322 (59/233)	1.02E-08
Cyclin-dependent kinase 11B (CDK11B)	PF00069	25.789 (49/190)	1.18E-08
Dual-specificity tyrosine-phosphorylation regulated kinase 3 (DYRK3)	PF00069	27.049 (66/244)	1.31E-08
Cyclin-dependent kinase 9 (CDK9)	PF00069	24.895 (59/237)	1.46E-08
Proto-oncogene serine/threonine-protein kinase mos (MOS)	PF00069	22.759 (66/290)	1.56E-08
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (PHKG1)	PF00069	31.250 (40/128)	1.78E-08
Serine/threonine-protein kinase D2 (PRKD2)	PF00130 ; PF00069	23.744 (52/219)	1.91E-08
Serine/threonine-protein kinase Nek9 (NEK9)	PF00069 ; PF00415	25.581 (55/215)	2.53E-08
Obscurin (OBSCN)	PF00041 ; PF07679 ; PF00612 ; PF00069 ; PF00621 More >>	25.000 (72/288)	3.37E-08
Checkpoint kinase-1 (CHK1)	PF00069	24.096 (60/249)	3.90E-08
Myosin light chain kinase family member 4 (MYLK4)	PF00069	22.176 (53/239)	4.04E-08
Bone morphogenetic protein receptor (BMPR2)	PF01064 ; PF00069	25.676 (57/222)	4.04E-08
Serine/threonine-protein kinase tousled-like 1 (TLK1)	PF00069	24.402 (51/209)	4.37E-08
Protein kinase C gamma (PRKCG)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	24.111 (61/253)	4.41E-08
Activin receptor type IIA (ACVR2A)	PF01064 ; PF00069	26.000 (52/200)	4.80E-08
PAK-4 protein kinase (PAK4)	PF00786 ; PF00069	25.106 (59/235)	5.60E-08
Doublecortin-like kinase 3 (DCLK3)	PF00069	25.140 (45/179)	5.65E-08
Rho-associated protein kinase 1 (ROCK1)	PF00069 ; PF08912	25.688 (56/218)	5.94E-08
IL-1 receptor-associated kinase 3 (IRAK3)	PF00531 ; PF00069	21.886 (65/297)	7.87E-08
Protein kinase C epsilon (PRKCE)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	23.830 (56/235)	8.74E-08
Testis-specific serine/threonine-protein kinase 6 (TSSK6)	PF00069	25.676 (57/222)	1.16E-07
Maternal embryonic leucine zipper kinase (MELK)	PF02149 ; PF00069	22.624 (50/221)	1.45E-07
MAPK/MAK/MRK overlapping kinase (MOK)	PF00069	23.502 (51/217)	1.51E-07
Apoptosis signal-regulating kinase 2 (MAP3K6)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	23.504 (55/234)	1.96E-07
Serine/threonine-protein kinase PLK3 (PLK3)	PF00069 ; PF00659	22.128 (52/235)	2.11E-07
Serine/threonine-protein kinase D3 (PRKD3)	PF00130 ; PF00169 ; PF00069 More >>	23.684 (54/228)	2.43E-07
Peripheral plasma membrane protein CASK (CASK)	PF00625 ; PF02828 ; PF00595 ; PF00069 ; PF00018 More >>	25.150 (42/167)	3.12E-07
Serine/threonine-protein kinase Sgk3 (SGK3)	PF00069 ; PF00433 ; PF00787 More >>	22.870 (51/223)	3.41E-07
Stress-activated protein kinase JNK3 (JNK3)	PF00069	24.194 (60/248)	3.41E-07
Rho-associated protein kinase 2 (ROCK2)	PF00069 ; PF08912	26.667 (44/165)	3.73E-07
Myosin light kinase (MYLK)	PF16620 ; PF00041 ; PF07679 ; PF00069 More >>	24.074 (52/216)	3.78E-07
Ribosomal protein S6 kinase-related protein (RSKR)	PF00069	28.972 (31/107)	3.83E-07
Stress-activated protein kinase JNK1 (JNK1)	PF00069	23.887 (59/247)	4.12E-07
Testis-specific serine/threonine-protein kinase 1 (TSSK1B)	PF00069	24.034 (56/233)	4.40E-07
Protein kinase C eta type (PRKCH)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	23.529 (56/238)	5.05E-07
Apoptosis signal-regulating kinase 1 (MAP3K5)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	26.554 (47/177)	5.65E-07
BR serine/threonine kinase 2 (BRSK2)	PF00069	27.273 (48/176)	6.18E-07
Protein kinase D (PRKD1)	PF00130 ; PF00169 ; PF00069 More >>	23.246 (53/228)	6.36E-07
Tyrosine-protein kinase EIF2AK2 (p68)	PF00035 ; PF00069	32.609 (30/92)	6.90E-07
Dual specificity mitogen-activated protein kinase kinase 6 (MAP2K6)	PF00069	23.735 (61/257)	7.79E-07
BR serine/threonine kinase 1 (BRSK1)	PF00069	25.116 (54/215)	8.22E-07
Protein kinase N3 (PKN3)	PF02185 ; PF00069 ; PF00433 More >>	25.957 (61/235)	9.11E-07
Serine/threonine-protein kinase 35 (STK35)	PF00069	27.684 (49/177)	1.03E-06
Mitogen-activated protein kinase 13 (MAPK13)	PF00069	28.000 (42/150)	1.22E-06
Serine/threonine-protein kinase STK11 (STK11)	PF00069	26.744 (46/172)	1.28E-06
Homeodomain-interacting protein kinase 3 (HIPK3)	PF00069	22.870 (51/223)	1.46E-06
Serine/threonine-protein kinase PDIK1L (PDIK1L)	PF00069	24.031 (62/258)	1.59E-06
Beta-adrenergic receptor kinase 2 (ADRBK2)	PF00169 ; PF00069 ; PF00615 More >>	23.394 (51/218)	1.66E-06
Stress-activated protein kinase JNK2 (JNK2)	PF00069	23.936 (45/188)	1.81E-06
Ribosomal protein S6 kinase beta-1 (S6K1)	PF00069 ; PF00433	22.685 (49/216)	1.88E-06
Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3)	PF00069	25.424 (75/295)	1.96E-06
Dual-specificity tyrosine-phosphorylation regulated kinase 1B (DYRK1B)	PF00069	27.979 (54/193)	1.98E-06
Serine/threonine-protein kinase Sgk2 (SGK2)	PF00069 ; PF00433	20.930 (45/215)	2.10E-06
Phosphorylase kinase testis gamma 2 (PHKG2)	PF00069	23.853 (52/218)	2.18E-06
Polo-like kinase 2 (PLK2)	PF00069 ; PF00659	21.811 (53/243)	2.18E-06
Homeodomain interacting protein kinase 2 (HIPK2)	PF00069	22.667 (51/225)	2.20E-06
Dual-specificity tyrosine-phosphorylation regulated kinase 4 (DYRK4)	PF00069	26.724 (62/232)	2.30E-06
TRAF2 and NCK interacting kinase (TNIK)	PF00780 ; PF00069	21.923 (57/260)	2.45E-06
Homeodomain-interacting protein kinase 1 (HIPK1)	PF00069	22.667 (51/225)	2.63E-06
NIMA-related kinase 2 (NEK2)	PF00069	24.405 (41/168)	2.98E-06
Misshapen-like kinase 1 (MINK1)	PF00780 ; PF00069	21.839 (57/261)	3.85E-06
Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5)	PF00780 ; PF00069	21.586 (49/227)	4.09E-06
Calcium/calmodulin-dependent protein kinase type IV (CAMK4)	PF00069	22.907 (52/227)	5.36E-06
Aurora kinase B (AURKB)	PF00069	25.000 (54/216)	5.53E-06
Citron Rho-interacting kinase (CIT)	PF00780 ; PF00169 ; PF00069 More >>	24.091 (53/220)	6.50E-06
Protein kinase N2 (PKN2)	PF02185 ; PF00069 ; PF00433 More >>	25.210 (60/238)	7.28E-06
Serine/threonine-protein kinase Nek10 (NEK10)	PF00069	22.414 (39/174)	8.22E-06
Serine/threonine-protein kinase greatwall (MASTL)	PF00069	25.405 (47/185)	9.20E-06
Ribosomal protein S6 kinase beta-2 (RPS6KB2)	PF00069 ; PF00433	23.288 (51/219)	1.03E-05
Nik-related protein kinase (NRK)	PF00780 ; PF00069	27.737 (38/137)	1.08E-05
Rhodopsin kinase GRK7 (GRK7)	PF00069 ; PF00615	25.000 (29/116)	1.10E-05
Eukaryotic translation initiation factor 2-alpha kinase 4 (EIF2AK4)	PF12745 ; PF00069 ; PF05773 ; PF13393 More >>	26.087 (36/138)	1.35E-05
ERK activator kinase 7 (MAP2K7)	PF00069	23.656 (44/186)	1.36E-05
Striated muscle preferentially expressed protein kinase (SPEG)	PF07679 ; PF00069 ; PF16650 More >>	26.267 (57/217)	1.55E-05
Ribosomal protein S6 kinase alpha-5 (RSK5)	PF00069 ; PF00433	21.659 (47/217)	1.74E-05
Protein kinase G2 (PRKG2)	PF00027 ; PF00069	22.685 (49/216)	1.84E-05
Calcium/calmodulin-dependent protein kinase type II subunit gamma (CAMK2G)	PF08332 ; PF00069	23.721 (51/215)	2.03E-05
Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A)	PF00069	26.754 (61/228)	2.07E-05
Inhibitor of nuclear factor kappa-B kinase subunit epsilon (IKBKE)	PF00069 ; PF18394 ; PF18396 More >>	26.316 (50/190)	2.14E-05
Serine/threonine-protein kinase PRP4 homolog (PRPF4B)	PF00069	25.248 (51/202)	2.23E-05
Beta-adrenergic receptor kinase 1 (ADRBK1)	PF00169 ; PF00069 ; PF00615 More >>	24.260 (41/169)	2.38E-05
Serine/threonine-protein kinase pim-2 (PIM2)	PF00069	22.222 (48/216)	2.43E-05
Triple functional domain protein (TRIO)	PF00650 ; PF07679 ; PF00169 ; PF00069 ; PF00621 ; PF16609 ; PF00018 ; PF00435 More >>	24.885 (54/217)	2.49E-05
MAPK-activated protein kinase 5 (MAPKAPK5)	PF00069	24.865 (46/185)	2.67E-05
Serine/threonine-protein kinase 32A (STK32A)	PF00069	20.732 (51/246)	2.98E-05
MEK kinase kinase 4 (MAP4K4)	PF00780 ; PF00069	23.810 (35/147)	3.18E-05
Serine/threonine-protein kinase NIK (MAP3K14)	PF00069	21.667 (52/240)	3.25E-05
Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4)	PF00069	22.134 (56/253)	3.47E-05
Ribosomal protein S6 kinase alpha-4 (RPS6KA4)	PF00069 ; PF00433	24.180 (59/244)	3.91E-05
Serine/threonine-protein kinase Chk2 (RAD53)	PF00498 ; PF00069	24.413 (52/213)	4.69E-05
TBC domain-containing protein kinase-like protein (TBCK)	PF00069 ; PF00566 ; PF00581 More >>	28.205 (33/117)	4.86E-05
Protein kinase C zeta (PRKCZ)	PF00130 ; PF00564 ; PF00069 ; PF00433 More >>	23.810 (35/147)	5.23E-05
Protein kinase C iota (PRKCI)	PF00130 ; PF00564 ; PF00069 ; PF00433 More >>	23.973 (35/146)	6.33E-05
Myosin-IIIa (MYO3A)	PF00612 ; PF00063 ; PF00069 More >>	24.498 (61/249)	6.34E-05
Protein kinase N1 (PKN1)	PF02185 ; PF00069 ; PF00433 More >>	25.620 (62/242)	6.74E-05
Yet another novel kinase 2 (STK32B)	PF00069	21.687 (36/166)	7.59E-05
Calcium/calmodulin-dependent protein kinase type II subunit alpha (CAMK2A)	PF08332 ; PF00069	23.721 (51/215)	1.31E-04
Large tumor suppressor homolog 2 (LATS2)	PF00069 ; PF00433	23.889 (43/180)	1.56E-04
Serine/threonine-protein kinase MRCK gamma (CDC42BPG)	PF00130 ; PF00780 ; PF08826 ; PF00069 More >>	23.154 (69/298)	2.15E-04
CDC42 binding protein kinase alpha (DMPK-like alpha)	PF00130 ; PF00780 ; PF08826 ; PF15796 ; PF00069 ; PF00433 More >>	25.571 (56/219)	2.37E-04
Casein kinase I gamma-1 (CSNK1G1)	PF12605 ; PF00069	27.619 (29/105)	3.44E-04
Interleukin-1 receptor-associated kinase-like 2 (IRAK2)	PF00531 ; PF00069	22.561 (37/164)	3.99E-04
Serine/threonine-protein kinase MRCK beta (CDC42BPB)	PF00130 ; PF00780 ; PF08826 ; PF15796 ; PF00069 More >>	24.096 (60/249)	4.15E-04
Eukaryotic translation initiation factor 2-alpha kinase 1 (EIF2AK1)	PF00069	26.994 (44/163)	5.39E-04
Serine/threonine-protein kinase LATS1 (LATS1)	PF00069 ; PF00627	23.243 (43/185)	8.14E-04
Protein kinase G1 (PRKG1)	PF00027 ; PF16808 ; PF00069 More >>	20.465 (44/215)	8.44E-04
PIM-3 protein kinase (PIM3)	PF00069	27.679 (31/112)	1.00E-03
Anti-mullerian hormone II receptor (AMHR2)	PF00069	21.739 (50/230)	1.00E-03
NDR2 protein kinase (STK38L)	PF00069 ; PF00433	21.229 (38/179)	1.00E-03
Membrane-associated kinase (PKMYT1)	PF00069	28.814 (34/118)	1.00E-03
Wee1-like protein kinase (WEE1)	PF00069	23.418 (37/158)	1.00E-03
Casein kinase I gamma-3 (CSNK1G3)	PF12605 ; PF00069	27.619 (29/105)	1.00E-03
NDR1 protein kinase (STK38)	PF00069 ; PF00433	21.788 (39/179)	1.00E-03
Calcium/calmodulin-dependent protein kinase type II subunit beta (CAMK2B)	PF08332 ; PF00069	22.791 (49/215)	2.00E-03
Activin receptor type IIB (ACVR2B)	PF01064 ; PF00069	21.675 (44/203)	2.00E-03
NF-kappa-B-activating kinase (TBK1)	PF00069 ; PF18394 ; PF18396 More >>	24.157 (43/178)	2.00E-03
Myosin-IIIb (MYO3B)	PF00612 ; PF00063 ; PF00069 More >>	29.545 (26/88)	2.00E-03
Sugen kinase 110 (SBK3)	PF00069	24.434 (54/221)	3.00E-03
CaM kinase-like vesicle-associated protein (CAMKV)	PF00069	23.684 (54/228)	4.00E-03
Polo-like kinase 1 (PLK1)	PF00069 ; PF00659	26.087 (24/92)	4.00E-03
Serine/threonine kinase-like domain-containing protein STKLD1 (STKLD1)	PF00069	24.638 (34/138)	4.00E-03
Casein kinase I delta (CSNK1D)	PF00069	24.138 (42/174)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins


Note: If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

References

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REF 1

Mutational Landscape of DDR2 Gene in Lung Squamous Cell Carcinoma Using Next-generation Sequencing. Clin Lung Cancer. 2018 Mar;19(2):163-169.e4.

REF 2

Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases. US9156852.

REF 3

DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome. ACS Chem Biol. 2019 Jan 18;14(1):37-49.

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