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Assay Detail

CHEMBL818491

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

Functional
Inhibition of glycoprotein IIb/III integrin mediated fibrinogen binding to activated platelets
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.
Hartman GD, Duggan ME, Hoffman WF, Meissner RJ, Perkins JJ, Zartman AE, Naylor-Olsen AM, Cook JJ, Glass JD, Lynch RJ, Zhang G, Gould RJ.
Bioorg Med Chem Lett (1999) 9 : 863 -868
PubMed 10206551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.56 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169158 1 7.89
CHEMBL326492 1 7.77
CHEMBL172674 1 7.64
CHEMBL171105 1 7.47
CHEMBL434303 1 7.26
CHEMBL440743 1 6.96
CHEMBL168711 1 6.89
CHEMBL172737 1 6.57
CHEMBL168466 1 6.42
CHEMBL354258 1 5.55
CHEMBL369858 1 5.31
CHEMBL166344 1 5.04
CHEMBL168440 1 4.54
CHEMBL171935 1 -
CHEMBL168391 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169158 IC50 = 13.0 nM 7.89
CHEMBL326492 IC50 = 17.0 nM 7.77
CHEMBL172674 IC50 = 23.0 nM 7.64
CHEMBL171105 IC50 = 34.0 nM 7.47
CHEMBL434303 IC50 = 55.0 nM 7.26
CHEMBL440743 IC50 = 110.0 nM 6.96
CHEMBL168711 IC50 = 130.0 nM 6.89
CHEMBL172737 IC50 = 270.0 nM 6.57
CHEMBL168466 IC50 = 380.0 nM 6.42
CHEMBL354258 IC50 = 2800.0 nM 5.55
CHEMBL369858 IC50 = 4900.0 nM 5.31
CHEMBL166344 IC50 = 9200.0 nM 5.04
CHEMBL168440 IC50 = 29000.0 nM 4.54
CHEMBL171935 IC50 > 30000.0 nM -
CHEMBL168391 IC50 = 230000.0 nM -