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Assay Detail

CHEMBL860900

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

Binding
Average Binding Constant for VEGFR2; NA=Not Active at 10 uM
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
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 7.04 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 9.64
CHEMBL101253 VATALANIB 3.0 1 7.16
CHEMBL1336 SORAFENIB 4.0 1 7.03
CHEMBL388978 STAUROSPORINE 1 6.57
CHEMBL24828 VANDETANIB 4.0 1 6.33
CHEMBL103667 DORAMAPIMOD 2.0 1 5.50
CHEMBL607707 PELITINIB 2.0 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL14762 SELICICLIB 2.0 1 -
CHEMBL428690 ALVOCIDIB 3.0 1 -
CHEMBL554 LAPATINIB 4.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL1725279 SP-600125 1 -
CHEMBL941 IMATINIB 4.0 1 -
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL553 ERLOTINIB 4.0 1 -
CHEMBL31965 CANERTINIB 3.0 1 -
CHEMBL278041 SB-202190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 0.23 nM 9.64
CHEMBL101253 VATALANIB Kd = 70.0 nM 7.16
CHEMBL1336 SORAFENIB Kd = 93.0 nM 7.03
CHEMBL388978 STAUROSPORINE Kd = 270.0 nM 6.57
CHEMBL24828 VANDETANIB Kd = 470.0 nM 6.33
CHEMBL103667 DORAMAPIMOD Kd = 3200.0 nM 5.50
CHEMBL607707 PELITINIB Kd - -
CHEMBL124660 TANDUTINIB Kd - -
CHEMBL91829 RUBOXISTAURIN Kd - -
CHEMBL14762 SELICICLIB Kd - -
CHEMBL428690 ALVOCIDIB Kd - -
CHEMBL554 LAPATINIB Kd - -
CHEMBL10 SB-203580 Kd - -
CHEMBL119385 NEFLAMAPIMOD Kd - -
CHEMBL1725279 SP-600125 Kd - -
CHEMBL941 IMATINIB Kd - -
CHEMBL939 GEFITINIB Kd - -
CHEMBL553 ERLOTINIB Kd - -
CHEMBL31965 CANERTINIB Kd - -
CHEMBL278041 SB-202190 Kd - -