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Assay Detail

CHEMBL697020

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

Functional
The compound was tested in vivo for the inhibition of aggregation of human gel-filtered platelets(GFP)
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Integrin alpha-IIb/beta-3 (CHEMBL2093869)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Egbertson MS, Cook JJ, Bednar B, Prugh JD, Bednar RA, Gaul SL, Gould RJ, Hartman GD, Homnick CF, Holahan MA, Libby LA, Lynch JJ, Lynch RJ, Sitko GR, Stranieri MT, Vassallo LM.
J Med Chem (1999) 42 : 2409 -2421
PubMed 10395482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.72 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL79211 1 8.15
CHEMBL78570 1 8.15
CHEMBL293601 1 8.10
CHEMBL78760 1 8.10
CHEMBL78503 1 8.05
CHEMBL312113 1 8.00
CHEMBL80819 1 8.00
CHEMBL80432 1 7.96
CHEMBL916 TIROFIBAN 4.0 1 7.96
CHEMBL78517 1 7.89
CHEMBL78898 1 7.85
CHEMBL79294 1 7.82
CHEMBL78398 1 7.82
CHEMBL311048 1 7.82
CHEMBL1229688 1 7.72
CHEMBL310350 1 7.68
CHEMBL310964 1 7.64
CHEMBL32960 1 7.57
CHEMBL80381 1 7.50
CHEMBL2115074 1 7.44
CHEMBL312330 1 6.39
CHEMBL80307 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL79211 IC50 = 7.0 nM 8.15
CHEMBL78570 IC50 = 7.0 nM 8.15
CHEMBL293601 IC50 = 8.0 nM 8.10
CHEMBL78760 IC50 = 8.0 nM 8.10
CHEMBL78503 IC50 = 9.0 nM 8.05
CHEMBL312113 IC50 = 10.0 nM 8.00
CHEMBL80819 IC50 = 10.0 nM 8.00
CHEMBL80432 IC50 = 11.0 nM 7.96
CHEMBL916 TIROFIBAN IC50 = 11.0 nM 7.96
CHEMBL78517 IC50 = 13.0 nM 7.89
CHEMBL78898 IC50 = 14.0 nM 7.85
CHEMBL79294 IC50 = 15.0 nM 7.82
CHEMBL78398 IC50 = 15.0 nM 7.82
CHEMBL311048 IC50 = 15.0 nM 7.82
CHEMBL1229688 IC50 = 19.0 nM 7.72
CHEMBL310350 IC50 = 21.0 nM 7.68
CHEMBL310964 IC50 = 23.0 nM 7.64
CHEMBL32960 IC50 = 27.0 nM 7.57
CHEMBL80381 IC50 = 32.0 nM 7.50
CHEMBL2115074 IC50 = 36.0 nM 7.44
CHEMBL312330 IC50 = 410.0 nM 6.39
CHEMBL80307 IC50 = 500.0 nM 6.30