Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25005 | Target Info | |||
| Target Name | Tyrosine-protein kinase BTK (ATK) | ||||
| Synonyms |
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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| Target Type | Successful Target | ||||
| Gene Name | BTK | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
PF-06651600
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Phase 2/3 | Compound Info | ||
| Synonyms |
CBRJPFGIXUFMTM-WDEREUQCSA-N; 1792180-81-4; UNII-2OYE00PC25; 2OYE00PC25; PF06651600; 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one; GTPL9559; SCHEMBL16764638; BCP24778; EX-A2613; ZINC526061581; example 5 [WO2015083028]; ACN-040697; compound 11 [PMID: 28139931]; HY-100754; CS-0020243; 1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malonate; 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]prop-2-en-1-one
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| Activity |
Ki = 62300 nM
|
[1] | |||
| Compound Name |
4-Amino-8-(1-methyl-1H-pyrazole-4-yl)cinnoline-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3586443; BDBM50097397
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-Tert-butyl-N-[2-methyl-3-[6-[4-(morpholine-4-carbonyl)anilino]-9-(3-phenylpropyl)purin-2-yl]phenyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3263643; BDBM50012082
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-Tert-butyl-N-[3-[4-[4-(morpholine-4-carbonyl)anilino]pyrimidin-2-yl]phenyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3263316; BDBM50012064
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-Tert-butyl-N-[3-[4-[4-(morpholine-4-carbonyl)anilino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]phenyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3263317; BDBM50012065
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
6-Tert-butyl-8-fluoro-2-[[2-fluoro-5-(hydroxymethyl)-4-(2-oxo-1H-pyridin-4-yl)phenyl]methyl]phthalazin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3902517; SCHEMBL15721059
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| Activity |
IC50 = 52269.88 nM
|
[4] | |||
| Compound Name |
4-Amino-8-(4-Methylpyridin-3-Yl)cinnoline-3-Carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3586444; BDBM50097396; Q27454913; 4-Amino-8-(4-methyl-3-pyridyl)cinnoline-3-carboxamide; 4RV
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| Activity |
IC50 = 100000 nM
|
[2] | |||
| Compound Name |
6-Tert-butyl-8-fluoro-2-[[3-(hydroxymethyl)-4-(2-oxo-1H-pyridin-4-yl)phenyl]methyl]phthalazin-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3961094; SCHEMBL15720310
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-(9H-Purin-6-ylamino)-cyclohexanecarboxylic acid 3-chloro-benzylamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3929151; SCHEMBL16012890; BDBM250516; US9469644, 2; N-[(3-chlorophenyl)methyl]-3-(7H-purin-6-ylamino)cyclohexane-1-carboxamide
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| Activity |
IC50 = 100000 nM
|
[5] | |||
| Compound Name |
N-(3-(2-((4-Morpholinophenyl)amino)-5-(phenylamino)pyrimidin-4-yl)phenyl)acrylamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3685423; SCHEMBL14740394; BDBM120746; US8703767, 6; N-[3-[5-anilino-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]prop-2-enamide
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-Amino-8-(1H-indole-6-yl)cinnoline-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3586445; SCHEMBL15288088; BDBM50097395; 4-amino-8-(1H-indol-6-yl)cinnoline-3-carboxamide
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| Activity |
IC50 = 850000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. J Med Chem. 2017 Mar 9;60(5):1971-1993. | ||||
| REF 2 | Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase. J Med Chem. 2015 Jul 23;58(14):5437-44. | ||||
| REF 3 | Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. | ||||
| REF 4 | US patent application no. 9458105B2, Inhibitors of Bruton's tyrosine kinase | ||||
| REF 5 | US patent application no. 9469644B2, Inhibitors of Bruton's tyrosine kinase | ||||
| REF 6 | US patent application no. 8703767B2, Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors | ||||
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