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Assay Detail

CHEMBL1011002

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

Functional
Inhibition of VEGF-mediated proliferation of HMVEC after 72 hrs
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HMVEC
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M, Lapointe GR, Feucht PH, Warne RL, Heise CC, Menezes D, Aardalen K, Ye H, He M, Le V, Vora J, Jansen JM, Wernette-Hammond ME, Harris AL.
J Med Chem (2009) 52 : 278 -292
PubMed 19113866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 7.06 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495763 1 8.30
CHEMBL496763 1 8.00
CHEMBL495749 1 8.00
CHEMBL495762 1 7.92
CHEMBL522892 DOVITINIB 3.0 1 7.89
CHEMBL496762 1 7.77
CHEMBL496764 1 7.77
CHEMBL204427 1 7.72
CHEMBL495962 1 7.62
CHEMBL523071 1 7.60
CHEMBL498013 1 7.47
CHEMBL526658 1 7.43
CHEMBL523745 1 7.41
CHEMBL496150 1 7.38
CHEMBL498214 1 7.35
CHEMBL204426 1 7.29
CHEMBL498205 1 7.19
CHEMBL495984 1 7.14
CHEMBL383417 1 7.11
CHEMBL498347 1 7.10
CHEMBL526285 1 7.00
CHEMBL526507 1 6.92
CHEMBL498206 1 6.82
CHEMBL118440 1 6.62
CHEMBL449593 1 6.57
CHEMBL521552 1 6.55
CHEMBL498551 1 6.47
CHEMBL526836 1 6.38
CHEMBL377345 1 6.38
CHEMBL522732 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495763 EC50 = 5.0 nM 8.30
CHEMBL496763 EC50 = 10.0 nM 8.00
CHEMBL495749 EC50 = 10.0 nM 8.00
CHEMBL495762 EC50 = 12.0 nM 7.92
CHEMBL522892 DOVITINIB EC50 = 13.0 nM 7.89
CHEMBL496762 EC50 = 17.0 nM 7.77
CHEMBL496764 EC50 = 17.0 nM 7.77
CHEMBL204427 EC50 = 19.0 nM 7.72
CHEMBL495962 EC50 = 24.0 nM 7.62
CHEMBL523071 EC50 = 25.0 nM 7.60
CHEMBL498013 EC50 = 34.0 nM 7.47
CHEMBL526658 EC50 = 37.0 nM 7.43
CHEMBL523745 EC50 = 39.0 nM 7.41
CHEMBL496150 EC50 = 42.0 nM 7.38
CHEMBL498214 EC50 = 45.0 nM 7.35
CHEMBL204426 EC50 = 51.0 nM 7.29
CHEMBL498205 EC50 = 64.0 nM 7.19
CHEMBL495984 EC50 = 72.0 nM 7.14
CHEMBL383417 EC50 = 78.0 nM 7.11
CHEMBL498347 EC50 = 80.0 nM 7.10
CHEMBL526285 EC50 = 100.0 nM 7.00
CHEMBL526507 EC50 = 120.0 nM 6.92
CHEMBL498206 EC50 = 150.0 nM 6.82
CHEMBL118440 EC50 = 240.0 nM 6.62
CHEMBL449593 EC50 = 270.0 nM 6.57
CHEMBL521552 EC50 = 280.0 nM 6.55
CHEMBL498551 EC50 = 340.0 nM 6.47
CHEMBL377345 EC50 = 420.0 nM 6.38
CHEMBL526836 EC50 = 420.0 nM 6.38
CHEMBL522732 EC50 = 480.0 nM 6.32
CHEMBL495735 EC50 = 1100.0 nM 5.96
CHEMBL495529 EC50 = 2000.0 nM 5.70
CHEMBL498348 EC50 = 3300.0 nM 5.48
CHEMBL523571 EC50 = 4600.0 nM 5.34
CHEMBL496172 EC50 > 10000.0 nM -
CHEMBL496173 EC50 > 10000.0 nM -
CHEMBL495983 EC50 > 10000.0 nM -