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Assay Detail

CHEMBL683386

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

Binding
Inhibition of biotinylated fibrinogen binding to immobilized integrin GPIIb/IIIa
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
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 13 8.94 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421547 1 9.77
CHEMBL328528 1 9.68
CHEMBL329015 1 9.49
CHEMBL87728 ELAROFIBAN 2.0 1 9.44
CHEMBL88944 1 9.36
CHEMBL88826 1 9.32
CHEMBL329871 1 9.29
CHEMBL315008 1 9.28
CHEMBL314318 1 9.22
CHEMBL89424 1 8.87
CHEMBL315637 1 8.38
CHEMBL89249 1 7.74
CHEMBL89624 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421547 IC50 = 0.17 nM 9.77
CHEMBL328528 IC50 = 0.21 nM 9.68
CHEMBL329015 IC50 = 0.32 nM 9.49
CHEMBL87728 ELAROFIBAN IC50 = 0.36 nM 9.44
CHEMBL88944 IC50 = 0.44 nM 9.36
CHEMBL88826 IC50 = 0.48 nM 9.32
CHEMBL329871 IC50 = 0.51 nM 9.29
CHEMBL315008 IC50 = 0.53 nM 9.28
CHEMBL314318 IC50 = 0.6 nM 9.22
CHEMBL89424 IC50 = 1.36 nM 8.87
CHEMBL315637 IC50 = 4.2 nM 8.38
CHEMBL89249 IC50 = 18.3 nM 7.74
CHEMBL89624 IC50 = 440.0 nM 6.36