Target Information

Target General Information

Top

Target ID

T43415 (Former ID: TTDC00316)

Target Name

Tyrosine-protein kinase (PTK)

Synonyms

Protein-tyrosine kinase; PTK

Click to Show/Hide

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

Rheumatoid arthritis [ICD-11: FA20]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 1 Approved Drugs

Baricitinib

Drug Info

Approved

Rheumatoid arthritis

[1]

Clinical Trial Drug(s)

[+] 6 Clinical Trial Drugs

ASP-015K

Drug Info

Phase 3

Psoriasis vulgaris

[2], [3]

Masitinib

Drug Info

Phase 3

Amyotrophic lateral sclerosis

[4]

ATI-502

Drug Info

Phase 2

Atopic dermatitis

[5]

KD019

Drug Info

Phase 2

Non-small-cell lung cancer

[6]

LEO 124249

Drug Info

Phase 2

Asthma

[5], [7]

TD-1473

Drug Info

Phase 1

Ulcerative colitis

[7]

Discontinued Drug(s)

[+] 4 Discontinued Drugs

SDZ-LAP-977

Drug Info

Discontinued in Phase 2

Psoriasis vulgaris

[8]

PN-355

Drug Info

Discontinued in Phase 1

Human immunodeficiency virus-1 infection

[9]

AP-23588

Drug Info

Terminated

Osteoporosis

[10]

CLX-0301

Drug Info

Terminated

Diabetic complication

[11]

Mode of Action

[+] 1 Modes of Action

Inhibitor

[+] 19 Inhibitor drugs

Baricitinib

Drug Info

[1]

ASP-015K

Drug Info

[7]

Masitinib

Drug Info

[12]

ATI-502

Drug Info

[5]

KD019

Drug Info

[12], [13]

LEO 124249

Drug Info

[5]

TD-1473

Drug Info

[7]

Aminotriazolopyridine derivative 1

Drug Info

[14]

Imidazo[4,5-c]pyridine derivative 1

Drug Info

[14]

Imidazo[4,5-c]pyridine derivative 2

Drug Info

[14]

PMID27774822-Compound-Figure10CompoundA

Drug Info

[15]

PMID27774822-Compound-Figure10Example1

Drug Info

[15]

PMID27774824-Compound-Figure11Example1up

Drug Info

[14]

Ruxolitinib derivative 1

Drug Info

[14]

Tetra-cyclic compound 1

Drug Info

[14]

SDZ-LAP-977

Drug Info

[16]

PN-355

Drug Info

[17]

AP-23588

Drug Info

[18]

CLX-0301

Drug Info

[19]

Drug Property Profile of Target

Top

(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

Co-Targets

Top

Co-Targets

Co-Targets Info

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8315).

REF 3

ClinicalTrials.gov (NCT02308163) A Study to Evaluate Safety and Efficacy of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to DMARDs. U.S. National Institutes of Health.

REF 4

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 5

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 6

ClinicalTrials.gov (NCT01487174) KD019 Versus Erlotinib in Subjects With Stage IIIB/IV Non Small Cell Lung Cancer With Progression After First- or Second-Line Chemotherapy. U.S. National Institutes of Health.

REF 7

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 8

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004738)

REF 9

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005490)

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017871)

REF 11

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013358)

REF 12

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 13

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 14

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.

REF 15

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.

REF 16

Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications. Bioorg Med Chem. 2008 Aug 15;16(16):7552-60.

REF 17

WO patent application no. 2005,0502,03, Biological materials and uses thereof.

REF 18

Foye's Principles of Medicinal Chemistry, Thomas L. Lemke, David A. Williams. 2008. Page(950).

REF 19

CLX-0901 (Calyx Therapeutics). Curr Opin Investig Drugs. 2001 May;2(5):650-3.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Feng ZHU

Prof. Yuzong CHEN