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Assay Detail

CHEMBL876415

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

Functional
Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type UCLAP-3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha-V/beta-5 (CHEMBL2096675)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
Goodman SL, Hölzemann G, Sulyok GA, Kessler H.
J Med Chem (2002) 45 : 1045 -1051
PubMed 11855984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.12 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429876 CILENGITIDE 3.0 1 6.40
CHEMBL9737 1 5.92
CHEMBL2372331 1 5.89
CHEMBL9200 1 5.70
CHEMBL2372407 1 5.68
CHEMBL268056 1 5.30
CHEMBL9508 1 4.75
CHEMBL267434 1 4.70
CHEMBL417426 1 4.68
CHEMBL417066 1 4.62
CHEMBL9555 1 4.58
CHEMBL9278 1 4.57
CHEMBL2372398 1 4.51
CHEMBL266151 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429876 CILENGITIDE IC50 = 400.0 nM 6.40
CHEMBL9737 IC50 = 1200.0 nM 5.92
CHEMBL2372331 IC50 = 1300.0 nM 5.89
CHEMBL9200 IC50 = 2000.0 nM 5.70
CHEMBL2372407 IC50 = 2100.0 nM 5.68
CHEMBL268056 IC50 = 5000.0 nM 5.30
CHEMBL9508 IC50 = 18000.0 nM 4.75
CHEMBL267434 IC50 = 20000.0 nM 4.70
CHEMBL417426 IC50 = 21000.0 nM 4.68
CHEMBL417066 IC50 = 24000.0 nM 4.62
CHEMBL9555 IC50 = 26000.0 nM 4.58
CHEMBL9278 IC50 = 27000.0 nM 4.57
CHEMBL2372398 IC50 = 31000.0 nM 4.51
CHEMBL266151 IC50 = 43000.0 nM 4.37