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Assay Detail

CHEMBL866446

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

Binding
Inhibition of Integrin alphav-beta6 receptor expressed in HT29 cell line
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 7 — Homologous single protein target
Curated By Expert

Target

Integrin alpha-V/beta-6 (CHEMBL2111416)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
Boys ML, Schretzman LA, Chandrakumar NS, Tollefson MB, Mohler SB, Downs VL, Penning TD, Russell MA, Wendt JA, Chen BB, Stenmark HG, Wu H, Spangler DP, Clare M, Desai BN, Khanna IK, Nguyen MN, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Steininger CN, Westlin M, Westlin W, Yu YX, Wang Y, Dalton CR, Norring SA.
Bioorg Med Chem Lett (2006) 16 : 839 -844
PubMed 16298127 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.60 6.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202295 1 6.31
CHEMBL202564 1 5.80
CHEMBL381663 1 5.62
CHEMBL369981 1 5.58
CHEMBL434191 1 5.57
CHEMBL202397 1 5.52
CHEMBL203690 1 5.43
CHEMBL202081 1 5.36
CHEMBL204259 1 5.21
CHEMBL202531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202295 IC50 = 486.0 nM 6.31
CHEMBL202564 IC50 = 1590.0 nM 5.80
CHEMBL381663 IC50 = 2420.0 nM 5.62
CHEMBL369981 IC50 = 2660.0 nM 5.58
CHEMBL434191 IC50 = 2670.0 nM 5.57
CHEMBL202397 IC50 = 3020.0 nM 5.52
CHEMBL203690 IC50 = 3730.0 nM 5.43
CHEMBL202081 IC50 = 4360.0 nM 5.36
CHEMBL204259 IC50 = 6240.0 nM 5.21
CHEMBL202531 IC50 > 10000.0 nM -