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Assay Detail

CHEMBL865652

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

Binding
Inhibitory activity against VEGFR2
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vascular endothelial growth factor receptor 2 (CHEMBL3337)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.
Frazier K, Jazan E, McBride CM, Pecchi S, Renhowe PA, Shafer CM, Taylor C, Bussiere D, He MM, Jansen JM, Lapointe G, Ma S, Vora J, Wiesmann M.
Bioorg Med Chem Lett (2006) 16 : 2247 -2251
PubMed 16446087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.40 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205893 1 9.00
CHEMBL205108 1 8.70
CHEMBL383618 1 8.52
CHEMBL204426 1 8.40
CHEMBL380702 1 8.10
CHEMBL204985 1 7.92
CHEMBL204427 1 7.89
CHEMBL204727 1 7.80
CHEMBL204524 1 7.62
CHEMBL383417 1 7.60
CHEMBL205405 1 7.48
CHEMBL381283 1 7.24
CHEMBL205406 1 6.96
CHEMBL377345 1 6.94
CHEMBL206410 1 6.78
CHEMBL205305 1 6.29
CHEMBL383299 1 6.26
CHEMBL207061 1 5.52
CHEMBL383261 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205893 IC50 = 1.0 nM 9.00
CHEMBL205108 IC50 = 2.0 nM 8.70
CHEMBL383618 IC50 = 3.0 nM 8.52
CHEMBL204426 IC50 = 4.0 nM 8.40
CHEMBL380702 IC50 = 8.0 nM 8.10
CHEMBL204985 IC50 = 12.0 nM 7.92
CHEMBL204427 IC50 = 13.0 nM 7.89
CHEMBL204727 IC50 = 16.0 nM 7.80
CHEMBL204524 IC50 = 24.0 nM 7.62
CHEMBL383417 IC50 = 25.0 nM 7.60
CHEMBL205405 IC50 = 33.0 nM 7.48
CHEMBL381283 IC50 = 57.0 nM 7.24
CHEMBL205406 IC50 = 109.0 nM 6.96
CHEMBL377345 IC50 = 114.0 nM 6.94
CHEMBL206410 IC50 = 168.0 nM 6.78
CHEMBL205305 IC50 = 507.0 nM 6.29
CHEMBL383299 IC50 = 552.0 nM 6.26
CHEMBL207061 IC50 = 3000.0 nM 5.52
CHEMBL383261 IC50 = 3000.0 nM 5.52