Assay Detail

CHEMBL860646

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Binding

Average Binding Constant for BIKE; NA=Not Active at 10 uM

ChEMBL ↗

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Target

BMP-2-inducible protein kinase (CHEMBL4522) ↗

Open DB target context

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BMP-2-inducible protein kinase (CHEMBL4522) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target BMP-2-inducible protein kinase

CHEMBL4522

Anchored from Assay target.

Protein identity BMP-2-inducible protein kinase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Expert

Target

BMP-2-inducible protein kinase (CHEMBL4522) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

A small molecule-kinase interaction map for clinical kinase inhibitors.

Fabian MA, Biggs WH, Treiber DK, Atteridge CE, Azimioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen PT, Floyd M, Ford JM, Galvin M, Gerlach JL, Grotzfeld RM, Herrgard S, Insko DE, Insko MA, Lai AG, Lélias JM, Mehta SA, Milanov ZV, Velasco AM, Wodicka LM, Patel HK, Zarrinkar PP, Lockhart DJ.
Nat Biotechnol (2005) 23 : 329 -336
PubMed 15711537 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	20	6.70	8.43

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL388978	STAUROSPORINE	—	1	8.43
CHEMBL1725279	SP-600125	—	1	7.60
CHEMBL535	SUNITINIB	4.0	1	7.42
CHEMBL607707	PELITINIB	2.0	1	6.27
CHEMBL31965	CANERTINIB	3.0	1	5.80
CHEMBL553	ERLOTINIB	4.0	1	5.75
CHEMBL91829	RUBOXISTAURIN	3.0	1	5.60
CHEMBL554	LAPATINIB	4.0	1	-
CHEMBL24828	VANDETANIB	4.0	1	-
CHEMBL939	GEFITINIB	4.0	1	-
CHEMBL941	IMATINIB	4.0	1	-
CHEMBL101253	VATALANIB	3.0	1	-
CHEMBL103667	DORAMAPIMOD	2.0	1	-
CHEMBL119385	NEFLAMAPIMOD	2.0	1	-
CHEMBL10	SB-203580	—	1	-
CHEMBL278041	SB-202190	—	1	-
CHEMBL124660	TANDUTINIB	2.0	1	-
CHEMBL428690	ALVOCIDIB	3.0	1	-
CHEMBL14762	SELICICLIB	2.0	1	-
CHEMBL1336	SORAFENIB	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL388978	STAUROSPORINE	Kd	=	3.7	nM	8.43
CHEMBL1725279	SP-600125	Kd	=	25.0	nM	7.60
CHEMBL535	SUNITINIB	Kd	=	38.0	nM	7.42
CHEMBL607707	PELITINIB	Kd	=	540.0	nM	6.27
CHEMBL31965	CANERTINIB	Kd	=	1600.0	nM	5.80
CHEMBL553	ERLOTINIB	Kd	=	1800.0	nM	5.75
CHEMBL91829	RUBOXISTAURIN	Kd	=	2500.0	nM	5.60
CHEMBL554	LAPATINIB	Kd		-	—	-
CHEMBL24828	VANDETANIB	Kd		-	—	-
CHEMBL939	GEFITINIB	Kd		-	—	-
CHEMBL941	IMATINIB	Kd		-	—	-
CHEMBL101253	VATALANIB	Kd		-	—	-
CHEMBL103667	DORAMAPIMOD	Kd		-	—	-
CHEMBL119385	NEFLAMAPIMOD	Kd		-	—	-
CHEMBL10	SB-203580	Kd		-	—	-
CHEMBL278041	SB-202190	Kd		-	—	-
CHEMBL124660	TANDUTINIB	Kd		-	—	-
CHEMBL428690	ALVOCIDIB	Kd		-	—	-
CHEMBL14762	SELICICLIB	Kd		-	—	-
CHEMBL1336	SORAFENIB	Kd		-	—	-