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Assay Detail

CHEMBL914744

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

Binding
Inhibition of human KDR kinase by HTRF assay
ChEMBL ↗
52
Total Activities
52
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

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ.
J Med Chem (2007) 50 : 2011 -2029
PubMed 17425296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.29 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225311 — — 1 8.52
CHEMBL390353 — — 1 8.30
CHEMBL223971 — — 1 8.30
CHEMBL390156 — — 1 8.22
CHEMBL225334 — — 1 8.15
CHEMBL225639 — — 1 8.10
CHEMBL225261 — — 1 8.05
CHEMBL387971 — — 1 8.00
CHEMBL225278 — — 1 7.96
CHEMBL223999 — — 1 7.96
CHEMBL224547 — — 1 7.96
CHEMBL225336 — — 1 7.96
CHEMBL224889 — — 1 7.70
CHEMBL375890 — — 1 7.66
CHEMBL225036 — — 1 7.64
CHEMBL224027 — — 1 7.62
CHEMBL225335 — — 1 7.52
CHEMBL224497 — — 1 7.48
CHEMBL225319 — — 1 7.44
CHEMBL426009 — — 1 7.44
CHEMBL224968 — — 1 7.42
CHEMBL223604 — — 1 7.40
CHEMBL224496 — — 1 7.38
CHEMBL374690 — — 1 7.38
CHEMBL390735 — — 1 7.36
CHEMBL376779 — — 1 7.35
CHEMBL214161 — — 1 7.32
CHEMBL445404 — — 1 7.32
CHEMBL223998 — — 1 7.32
CHEMBL375491 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225311 — IC50 = 3.0 nM 8.52
CHEMBL390353 — IC50 = 5.0 nM 8.30
CHEMBL223971 — IC50 = 5.0 nM 8.30
CHEMBL390156 — IC50 = 6.0 nM 8.22
CHEMBL225334 — IC50 = 7.0 nM 8.15
CHEMBL225639 — IC50 = 8.0 nM 8.10
CHEMBL225261 — IC50 = 9.0 nM 8.05
CHEMBL387971 — IC50 = 10.0 nM 8.00
CHEMBL225278 — IC50 = 11.0 nM 7.96
CHEMBL223999 — IC50 = 11.0 nM 7.96
CHEMBL224547 — IC50 = 11.0 nM 7.96
CHEMBL225336 — IC50 = 11.0 nM 7.96
CHEMBL224889 — IC50 = 20.0 nM 7.70
CHEMBL375890 — IC50 = 22.0 nM 7.66
CHEMBL225036 — IC50 = 23.0 nM 7.64
CHEMBL224027 — IC50 = 24.0 nM 7.62
CHEMBL225335 — IC50 = 30.0 nM 7.52
CHEMBL224497 — IC50 = 33.0 nM 7.48
CHEMBL225319 — IC50 = 36.0 nM 7.44
CHEMBL426009 — IC50 = 36.0 nM 7.44
CHEMBL224968 — IC50 = 38.0 nM 7.42
CHEMBL223604 — IC50 = 40.0 nM 7.40
CHEMBL224496 — IC50 = 42.0 nM 7.38
CHEMBL374690 — IC50 = 42.0 nM 7.38
CHEMBL390735 — IC50 = 44.0 nM 7.36
CHEMBL376779 — IC50 = 45.0 nM 7.35
CHEMBL445404 — IC50 = 48.0 nM 7.32
CHEMBL223998 — IC50 = 48.0 nM 7.32
CHEMBL214161 — IC50 = 48.0 nM 7.32
CHEMBL375491 — IC50 = 50.0 nM 7.30
CHEMBL223220 — IC50 = 51.0 nM 7.29
CHEMBL225193 — IC50 = 53.0 nM 7.28
CHEMBL223219 — IC50 = 54.0 nM 7.27
CHEMBL224918 — IC50 = 62.0 nM 7.21
CHEMBL213507 — IC50 = 61.0 nM 7.21
CHEMBL387972 — IC50 = 69.0 nM 7.16
CHEMBL223997 — IC50 = 75.0 nM 7.12
CHEMBL387929 — IC50 = 78.0 nM 7.11
CHEMBL225240 — IC50 = 84.0 nM 7.08
CHEMBL225090 — IC50 = 85.0 nM 7.07
CHEMBL225318 — IC50 = 101.0 nM 7.00
CHEMBL375692 — IC50 = 108.0 nM 6.97
CHEMBL224917 — IC50 = 124.0 nM 6.91
CHEMBL225248 — IC50 = 159.0 nM 6.80
CHEMBL224834 — IC50 = 195.0 nM 6.71
CHEMBL441369 — IC50 = 708.0 nM 6.15
CHEMBL434180 — IC50 = 962.0 nM 6.02
CHEMBL223943 — IC50 = 1000.0 nM 6.00
CHEMBL374627 — IC50 = 2370.0 nM 5.62
CHEMBL389499 — IC50 = 4680.0 nM 5.33