General Information of the Protein
Protein ID
PT01669
Protein Name
Cytoplasmic tyrosine-protein kinase BMX
Secondarily
Protein Name
Bone marrow tyrosine kinase gene in chromosome X protein
Epithelial and endothelial tyrosine kinase
NTK38
Gene Name
BMX
Sequence
MDTKSILEELLLKRSQQKKKMSPNNYKERLFVLTKTNLSYYEYDKMKRGSRKGSIEIKKIRCVEKVNLEEQTPVERQYPFQIVYKDGLLYVYASNEESRSQWLKALQKEIRGNPHLLVKYHSGFFVDGKFLCCQQSCKAAPGCTLWEAYANLHTAVNEEKHRVPTFPDRVLKIPRAVPVLKMDAPSSSTTLAQYDNESKKNYGSQPPSSSTSLAQYDSNSKKIYGSQPNFNMQYIPREDFPDWWQVRKLKSSSSSEDVASSNQKERNVNHTTSKISWEFPESSSSEEEENLDDYDWFAGNISRSQSEQLLRQKGKEGAFMVRNSSQVGMYTVSLFSKAVNDKKGTVKHYHVHTNAENKLYLAENYCFDSIPKLIHYHQHNSAGMITRLRHPVSTKANKVPDSVSLGNGIWELKREEITLLKELGSGQFGVVQLGKWKGQYDVAVKMIKEGSMSEDEFFQEAQTMMKLSHPKLVKFYGVCSKEYPIYIVTEYISNGCLLNYLRSHGKGLEPSQLLEMCYDVCEGMAFLESHQFIHRDLAARNCLVDRDLCVKVSDFGMTRYVLDDQYVSSVGTKFPVKWSAPEVFHYFKYSSKSDVWAFGILMWEVFSLGKQPYDLYDNSQVVLKVSQGHRLYRPHLASDTIYQIMYSCWHELPEKRPTFQQLLSSIEPLREKDKH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Tec family
Function
Non-receptor tyrosine kinase that plays central but diverse modulatory roles in various signaling processes involved in the regulation of actin reorganization, cell migration, cell proliferation and survival, cell adhesion, and apoptosis. Participates in signal transduction stimulated by growth factor receptors, cytokine receptors, G-protein coupled receptors, antigen receptors and integrins. Induces tyrosine phosphorylation of BCAR1 in response to integrin regulation. Activation of BMX by integrins is mediated by PTK2/FAK1, a key mediator of integrin signaling events leading to the regulation of actin cytoskeleton and cell motility. Plays a critical role in TNF-induced angiogenesis, and implicated in the signaling of TEK and FLT1 receptors, 2 important receptor families essential for angiogenesis. Required for the phosphorylation and activation of STAT3, a transcription factor involved in cell differentiation. Also involved in interleukin-6 (IL6) induced differentiation. Also plays a role in programming adaptive cytoprotection against extracellular stress in different cell systems, salivary epithelial cells, brain endothelial cells, and dermal fibroblasts. May be involved in regulation of endocytosis through its interaction with an endosomal protein RUFY1. May also play a role in the growth and differentiation of hematopoietic cells; as well as in signal transduction in endocardial and arterial endothelial cells.
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Uniprot ID
Primary ID:
P51813

Secondarily ID:
A6NIH9
O60564
Q12871
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Ensembl ID
ENSG00000102010
HGNC ID
HGNC:1079
Subcellular Location
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0387295
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl]pyrimidine-5-carboxamide
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C31H28F3N7O3
 1
1
GI50 = 8 nM
   TI
   LI
   LO
   TS
CP0389976
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
   Show/Hide
C31H28F3N7O3
 1
1
GI50 = 13 nM
   TI
   LI
   LO
   TS
CP0224766
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
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C33H35N7O6
 1
1
GI50 = 16 nM
   TI
   LI
   LO
   TS
CP0454874
2-fluoro-5-methyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C32H30FN7O3
 1
1
GI50 = 31 nM
   TI
   LI
   LO
   TS
CP0410349
N-[5-[(2-fluoro-5-methylbenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C31H30FN7O3
 1
1
GI50 = 44 nM
   TI
   LI
   LO
   TS
CP0387299
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
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C31H30F3N7O3
 1
1
GI50 = 85 nM
   TI
   LI
   LO
   TS
CP0407916
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl]pyrimidine-5-carboxamide
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C33H35N7O6
 1
1
GI50 = 98 nM
   TI
   LI
   LO
   TS
CP0407915
N-[5-[(3,5-dimethoxybenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C32H33N7O5
 1
1
GI50 = 119 nM
   TI
   LI
   LO
   TS
CP0451734
(2S)-2-amino-4-methyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]pentanamide
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C30H36N8O3
 1
1
GI50 = 130 nM
   TI
   LI
   LO
   TS
CP0569060
N-[5-(2,3-dihydro-1,4-benzodioxine-6-carbonylamino)-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C32H31N7O5
 1
1
GI50 = 155 nM
   TI
   LI
   LO
   TS
CP0410352
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-1,3-benzodioxole-5-carboxamide
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C32H29N7O5
 1
1
GI50 = 230 nM
   TI
   LI
   LO
   TS
CP0454872
3,4-dimethoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C33H33N7O5
 1
1
GI50 = 240 nM
   TI
   LI
   LO
   TS
CP0065873
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C26H29N7O2
 1
1
GI50 = 280 nM
   TI
   LI
   LO
   TS
CP0387298
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
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C33H37N7O6
 1
1
GI50 = 610 nM
   TI
   LI
   LO
   TS
CP0555770
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-4-propylcyclohexane-1-carboxamide
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C34H41N7O3
 1
1
GI50 = 640 nM
   TI
   LI
   LO
   TS
CP0573876
N-[5-[(2-methoxybenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C31H31N7O4
 1
1
GI50 = 670 nM
   TI
   LI
   LO
   TS
CP0458266
3,5-dimethoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C33H33N7O5
 1
1
GI50 = 690 nM
   TI
   LI
   LO
   TS
CP0394713
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3,5-bis(trifluoromethyl)benzamide
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C33H27F6N7O3
 1
1
GI50 = 780 nM
   TI
   LI
   LO
   TS
CP0407912
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-5,6,7,8-tetrahydronaphthalene-2-carboxamide
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C35H35N7O3
 1
1
GI50 = 860 nM
   TI
   LI
   LO
   TS
CP0560243
N-[5-[(3,4-dimethoxybenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C32H33N7O5
 1
1
GI50 = 1000 nM
   TI
   LI
   LO
   TS
CP0552358
4-(dimethylamino)-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C33H34N8O3
 1
1
GI50 = 1030 nM
   TI
   LI
   LO
   TS
CP0407911
4-methoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C32H31N7O4
 1
1
GI50 = 1070 nM
   TI
   LI
   LO
   TS
CP0447647
N-[5-(1,3-benzodioxole-5-carbonylamino)-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C31H29N7O5
 1
1
GI50 = 1080 nM
   TI
   LI
   LO
   TS
CP0451735
N-[5-[(4-methoxybenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C31H31N7O4
 1
1
GI50 = 1100 nM
   TI
   LI
   LO
   TS
CP0573874
4-methyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide
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C33H30F3N7O3
 1
1
GI50 = 1240 nM
   TI
   LI
   LO
   TS
CP0573875
4-methyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]cyclohexane-1-carboxamide
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C32H37N7O3
 1
1
GI50 = 2280 nM
   TI
   LI
   LO
   TS
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 = 2340 nM
   TI
   LI
   LO
   TS
CP0410348
4-butyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]cyclohexane-1-carboxamide
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C35H43N7O3
 1
1
GI50 = 2490 nM
   TI
   LI
   LO
   TS
CP0454873
2,4-dimethoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C33H33N7O5
 1
1
GI50 = 2740 nM
   TI
   LI
   LO
   TS
CP0555769
2-fluoro-6-methyl-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
   Show/Hide
C32H30FN7O3
 1
1
GI50 = 2780 nM
   TI
   LI
   LO
   TS
CP0410351
2,5-dimethoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
   Show/Hide
C33H33N7O5
 1
1
GI50 = 3000 nM
   TI
   LI
   LO
   TS
CP0570219
2-methoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
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C32H31N7O4
 1
1
GI50 = 3010 nM
   TI
   LI
   LO
   TS
CP0559026
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-4-propan-2-ylcyclohexane-1-carboxamide
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C34H41N7O3
 1
1
GI50 = 5280 nM
   TI
   LI
   LO
   TS
CP0569057
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-4-(trifluoromethyl)cyclohexane-1-carboxamide
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C32H34F3N7O3
 1
1
GI50 = 5900 nM
   TI
   LI
   LO
   TS
CP0451732
3,4,5-trimethoxy-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]benzamide
   Show/Hide
C34H35N7O6
 1
1
GI50 = 5930 nM
   TI
   LI
   LO
   TS
CP0569058
N-[5-[(3-methoxybenzoyl)amino]-2-methylphenyl]-4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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C31H31N7O4
 1
1
GI50 = 6000 nM
   TI
   LI
   LO
   TS
CP0407914
tert-butyl (4S)-4-amino-5-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]anilino]-5-oxopentanoate
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C33H40N8O5
 1
1
GI50 = 8350 nM
   TI
   LI
   LO
   TS
CP0407913
(2S)-2-amino-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-phenylpropanamide
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C33H34N8O3
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0451733
(2S)-2-amino-3-(1H-indol-2-yl)-N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]propanamide
   Show/Hide
C35H35N9O3
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0573873
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide
   Show/Hide
C33H31N7O5
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0019908
BDBM50242742
   Show/Hide
C30H40ClN7O3S
 1
1
IC50 = 1578 nM
   TI
   LI
   LO
   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
   Show/Hide
C27H28FN7O2
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
   Show/Hide
C26H34Cl2N7O7P
 1
1
IC50 = 3405 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
   Show/Hide
C26H27FN6O
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
   Show/Hide
C17H18N4O2
 1
1
IC50 = 6900 nM
   TI
   LI
   LO
   TS
CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
   Show/Hide
C20H15N5
 1
1
IC50 = 9700 nM
   TI
   LI
   LO
   TS
CP0395047
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine
   Show/Hide
C21H18FN5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
   Show/Hide
C17H18N4O
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
   Show/Hide
C23H26N6O3S
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
   Show/Hide
C26H29N5O3
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
   Show/Hide
C22H25FN6O2
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C28H32N6O5
 1
1
IC50 > 7400 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019908
BDBM50242742
   Show/Hide
C30H40ClN7O3S
 2
1 EC50 > 1000 nM
2 Kd = 1100 nM
CP0007430
IBRUTINIB
   Show/Hide
C25H24N6O2
 6
1 IC50 = 0.5 nM
2 IC50 = 0.8 nM
3 IC50 = 1 nM
4 IC50 = 5.8 nM
5 Kd = 1.4 nM
6 Kd = 1.6 nM
CP0060760
US9447106, 27b (peak 2)
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C27H29N5O3
 2
1 IC50 = 0.62 nM
2 Kd = 1600 nM
CP0113747
2-methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide
   Show/Hide
C29H23F3N6O3
 1
1 IC50 = 1.9 nM
CP0224766
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
   Show/Hide
C33H35N7O6
 1
1 IC50 = 11 nM
CP0086121
ACP-196
   Show/Hide
C26H23N7O2
 3
1 IC50 = 46 nM
2 Kd = 19 nM
3 Kd = 610 nM
CP0036058
N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide
   Show/Hide
C24H25ClFN5O3
 3
1 IC50 = 586 nM
2 Kd = 1200 nM
3 Kd = 2600 nM
CP0035025
4-anilinoquinazoline deriv. 2
   Show/Hide
C17H13BrN4O
 1
1 IC50 = 1100 nM
Clinical Information about the Protein
Target 1 ( Tyrosine-protein kinase BMX (BMX) )
Target Type Patented-recorded Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06169 Cytoplasmic tyrosine-protein kinase BMX Mus musculus, Mouse