Assay Detail

CHEMBL859868

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Binding

Average Binding Constant for ABL1; NA=Not Active at 10 uM

ChEMBL ↗

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Target

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗

Open DB target context

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Tyrosine-protein kinase ABL1 (CHEMBL1862) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase ABL1

CHEMBL1862

Anchored from Assay target.

Protein identity Tyrosine-protein kinase ABL1

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

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗

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	6.56	8.66

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL941	IMATINIB	4.0	1	8.66
CHEMBL1336	SORAFENIB	4.0	1	6.89
CHEMBL607707	PELITINIB	2.0	1	6.66
CHEMBL24828	VANDETANIB	4.0	1	6.57
CHEMBL31965	CANERTINIB	3.0	1	6.47
CHEMBL388978	STAUROSPORINE	—	1	6.39
CHEMBL553	ERLOTINIB	4.0	1	6.11
CHEMBL119385	NEFLAMAPIMOD	2.0	1	6.06
CHEMBL535	SUNITINIB	4.0	1	6.00
CHEMBL103667	DORAMAPIMOD	2.0	1	5.82
CHEMBL554	LAPATINIB	4.0	1	-
CHEMBL101253	VATALANIB	3.0	1	-
CHEMBL939	GEFITINIB	4.0	1	-
CHEMBL1725279	SP-600125	—	1	-
CHEMBL10	SB-203580	—	1	-
CHEMBL278041	SB-202190	—	1	-
CHEMBL428690	ALVOCIDIB	3.0	1	-
CHEMBL14762	SELICICLIB	2.0	1	-
CHEMBL124660	TANDUTINIB	2.0	1	-
CHEMBL91829	RUBOXISTAURIN	3.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL941	IMATINIB	Kd	=	2.2	nM	8.66
CHEMBL1336	SORAFENIB	Kd	=	130.0	nM	6.89
CHEMBL607707	PELITINIB	Kd	=	220.0	nM	6.66
CHEMBL24828	VANDETANIB	Kd	=	270.0	nM	6.57
CHEMBL31965	CANERTINIB	Kd	=	340.0	nM	6.47
CHEMBL388978	STAUROSPORINE	Kd	=	410.0	nM	6.39
CHEMBL553	ERLOTINIB	Kd	=	770.0	nM	6.11
CHEMBL119385	NEFLAMAPIMOD	Kd	=	870.0	nM	6.06
CHEMBL535	SUNITINIB	Kd	=	1000.0	nM	6.00
CHEMBL103667	DORAMAPIMOD	Kd	=	1500.0	nM	5.82
CHEMBL554	LAPATINIB	Kd		-	—	-
CHEMBL101253	VATALANIB	Kd		-	—	-
CHEMBL939	GEFITINIB	Kd		-	—	-
CHEMBL1725279	SP-600125	Kd		-	—	-
CHEMBL10	SB-203580	Kd		-	—	-
CHEMBL278041	SB-202190	Kd		-	—	-
CHEMBL428690	ALVOCIDIB	Kd		-	—	-
CHEMBL14762	SELICICLIB	Kd		-	—	-
CHEMBL124660	TANDUTINIB	Kd		-	—	-
CHEMBL91829	RUBOXISTAURIN	Kd		-	—	-