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Assay Detail

CHEMBL699520

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Functional
Inhibition of thrombin-induced human gel-filtered platelet aggregation
12
Total Activities
12
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

1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.
Lawson EC, Hoekstra WJ, Addo MF, Andrade-Gordon P, Damiano BP, Kauffman JA, Mitchell JA, Maryanoff BE.
Bioorg Med Chem Lett (2001) 11 : 2619 -2622
PubMed 11551763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 10.01 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315008 1 10.80
CHEMBL421547 1 10.57
CHEMBL329015 1 10.39
CHEMBL329871 1 10.37
CHEMBL88944 1 10.24
CHEMBL87728 ELAROFIBAN 2.0 1 10.22
CHEMBL328528 1 10.21
CHEMBL88826 1 10.17
CHEMBL89424 1 9.92
CHEMBL315637 1 9.43
CHEMBL314318 1 9.22
CHEMBL89249 1 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315008 IC50 = 0.016 nM 10.80
CHEMBL421547 IC50 = 0.027 nM 10.57
CHEMBL329015 IC50 = 0.041 nM 10.39
CHEMBL329871 IC50 = 0.043 nM 10.37
CHEMBL88944 IC50 = 0.057 nM 10.24
CHEMBL87728 ELAROFIBAN IC50 = 0.06 nM 10.22
CHEMBL328528 IC50 = 0.061 nM 10.21
CHEMBL88826 IC50 = 0.068 nM 10.17
CHEMBL89424 IC50 = 0.12 nM 9.92
CHEMBL315637 IC50 = 0.37 nM 9.43
CHEMBL314318 IC50 = 0.6 nM 9.22
CHEMBL89249 IC50 = 2.7 nM 8.57