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Assay Detail

CHEMBL1786465

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

Functional
Antagonist activity at alpha2bbeta3 integrin receptor
11
Total Activities
11
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

Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
Ishikawa M, Hashimoto Y.
J Med Chem (2011) 54 : 1539 -1554
PubMed 21344906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 9.33 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782661 1 10.64
CHEMBL1782660 1 9.74
CHEMBL599119 1 9.68
CHEMBL1782663 1 9.40
CHEMBL1083695 1 9.36
CHEMBL599138 1 9.25
CHEMBL1782662 1 9.11
CHEMBL1782659 1 9.03
CHEMBL1782657 1 9.01
CHEMBL1782658 1 8.92
CHEMBL598737 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782661 IC50 = 0.023 nM 10.64
CHEMBL1782660 IC50 = 0.18 nM 9.74
CHEMBL599119 IC50 = 0.21 nM 9.68
CHEMBL1782663 IC50 = 0.4 nM 9.40
CHEMBL1083695 IC50 = 0.44 nM 9.36
CHEMBL599138 IC50 = 0.56 nM 9.25
CHEMBL1782662 IC50 = 0.78 nM 9.11
CHEMBL1782659 IC50 = 0.94 nM 9.03
CHEMBL1782657 IC50 = 0.98 nM 9.01
CHEMBL1782658 IC50 = 1.2 nM 8.92
CHEMBL598737 IC50 = 3.0 nM 8.52