Assay Detail

CHEMBL860786

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Average Binding Constant for AAK1; NA=Not Active at 10 uM

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

AP2-associated protein kinase 1 (CHEMBL3830) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

AP2-associated protein kinase 1 (CHEMBL3830) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target AP2-associated protein kinase 1

CHEMBL3830

Anchored from Assay target.

Protein identity AP2-associated protein kinase 1

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

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

AP2-associated protein kinase 1 (CHEMBL3830) ↗

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	6.71	8.89

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL388978	STAUROSPORINE	—	1	8.89
CHEMBL1725279	SP-600125	—	1	7.46
CHEMBL535	SUNITINIB	4.0	1	6.89
CHEMBL91829	RUBOXISTAURIN	3.0	1	6.02
CHEMBL607707	PELITINIB	2.0	1	5.64
CHEMBL553	ERLOTINIB	4.0	1	5.36
CHEMBL101253	VATALANIB	3.0	1	-
CHEMBL124660	TANDUTINIB	2.0	1	-
CHEMBL1336	SORAFENIB	4.0	1	-
CHEMBL14762	SELICICLIB	2.0	1	-
CHEMBL428690	ALVOCIDIB	3.0	1	-
CHEMBL278041	SB-202190	—	1	-
CHEMBL10	SB-203580	—	1	-
CHEMBL119385	NEFLAMAPIMOD	2.0	1	-
CHEMBL103667	DORAMAPIMOD	2.0	1	-
CHEMBL941	IMATINIB	4.0	1	-
CHEMBL939	GEFITINIB	4.0	1	-
CHEMBL24828	VANDETANIB	4.0	1	-
CHEMBL554	LAPATINIB	4.0	1	-
CHEMBL31965	CANERTINIB	3.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL388978	STAUROSPORINE	Kd	=	1.3	nM	8.89
CHEMBL1725279	SP-600125	Kd	=	35.0	nM	7.46
CHEMBL535	SUNITINIB	Kd	=	130.0	nM	6.89
CHEMBL91829	RUBOXISTAURIN	Kd	=	960.0	nM	6.02
CHEMBL607707	PELITINIB	Kd	=	2300.0	nM	5.64
CHEMBL553	ERLOTINIB	Kd	=	4400.0	nM	5.36
CHEMBL101253	VATALANIB	Kd		-	—	-
CHEMBL124660	TANDUTINIB	Kd		-	—	-
CHEMBL1336	SORAFENIB	Kd		-	—	-
CHEMBL14762	SELICICLIB	Kd		-	—	-
CHEMBL428690	ALVOCIDIB	Kd		-	—	-
CHEMBL278041	SB-202190	Kd		-	—	-
CHEMBL10	SB-203580	Kd		-	—	-
CHEMBL119385	NEFLAMAPIMOD	Kd		-	—	-
CHEMBL103667	DORAMAPIMOD	Kd		-	—	-
CHEMBL941	IMATINIB	Kd		-	—	-
CHEMBL939	GEFITINIB	Kd		-	—	-
CHEMBL24828	VANDETANIB	Kd		-	—	-
CHEMBL554	LAPATINIB	Kd		-	—	-
CHEMBL31965	CANERTINIB	Kd		-	—	-