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Assay Detail

CHEMBL1839795

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

Binding
Displacement of FITC-labeled fibrinogen from alpha2beta3 in human platelets
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Integrin alpha-2/beta-3 (CHEMBL2111461)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor.
Krysko AA, Samoylenko GV, Polishchuk PG, Andronati SA, Kabanova TA, Khristova TM, Kuz'min VE, Kabanov VM, Krysko OL, Varnek AA, Grygorash RY.
Bioorg Med Chem Lett (2011) 21 : 5971 -5974
PubMed 21852128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.17 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836344 1 8.26
CHEMBL1836347 1 8.19
CHEMBL1836351 1 8.19
CHEMBL1836345 1 8.17
CHEMBL1836355 1 7.66
CHEMBL1836350 1 7.43
CHEMBL1836342 1 6.57
CHEMBL1836348 1 6.46
CHEMBL1836343 1 5.92
CHEMBL265628 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836344 IC50 = 5.5 nM 8.26
CHEMBL1836347 IC50 = 6.5 nM 8.19
CHEMBL1836351 IC50 = 6.5 nM 8.19
CHEMBL1836345 IC50 = 6.8 nM 8.17
CHEMBL1836355 IC50 = 22.0 nM 7.66
CHEMBL1836350 IC50 = 37.0 nM 7.43
CHEMBL1836342 IC50 = 270.0 nM 6.57
CHEMBL1836348 IC50 = 350.0 nM 6.46
CHEMBL1836343 IC50 = 1200.0 nM 5.92
CHEMBL265628 IC50 = 13000.0 nM 4.89