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Assay Detail

CHEMBL642138

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Functional
Alpha-5 beta-1 antagonism using an ELISA assay
18
Total Activities
18
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-5/beta-1 (CHEMBL2095226)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Smallheer JM, Weigelt CA, Woerner FJ, Wells JS, Daneker WF, Mousa SA, Wexler RR, Jadhav PK.
Bioorg Med Chem Lett (2004) 14 : 383 -387
PubMed 14698164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.03 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338439 1 9.74
CHEMBL126071 1 9.41
CHEMBL435806 1 8.85
CHEMBL126341 1 7.89
CHEMBL126983 1 7.85
CHEMBL338806 1 7.75
CHEMBL340309 1 7.68
CHEMBL339751 1 7.41
CHEMBL419795 1 6.77
CHEMBL126416 1 6.64
CHEMBL127133 1 6.51
CHEMBL127492 1 6.17
CHEMBL2111839 1 5.92
CHEMBL340703 1 5.82
CHEMBL338865 1 5.75
CHEMBL339476 1 5.57
CHEMBL127525 1 5.52
CHEMBL126925 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338439 IC50 = 0.18 nM 9.74
CHEMBL126071 IC50 = 0.39 nM 9.41
CHEMBL435806 IC50 = 1.4 nM 8.85
CHEMBL126341 IC50 = 13.0 nM 7.89
CHEMBL126983 IC50 = 14.0 nM 7.85
CHEMBL338806 IC50 = 18.0 nM 7.75
CHEMBL340309 IC50 = 21.0 nM 7.68
CHEMBL339751 IC50 = 39.0 nM 7.41
CHEMBL419795 IC50 = 170.0 nM 6.77
CHEMBL126416 IC50 = 230.0 nM 6.64
CHEMBL127133 IC50 = 310.0 nM 6.51
CHEMBL127492 IC50 = 670.0 nM 6.17
CHEMBL2111839 IC50 = 1200.0 nM 5.92
CHEMBL340703 IC50 = 1500.0 nM 5.82
CHEMBL338865 IC50 = 1800.0 nM 5.75
CHEMBL339476 IC50 = 2700.0 nM 5.57
CHEMBL127525 IC50 = 3000.0 nM 5.52
CHEMBL126925 IC50 = 4700.0 nM 5.33