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Assay Detail

CHEMBL4375379

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

Binding
Inhibition of integrin alphavbeta5 (unknown origin) by radioligand binding assay
2
Total Activities
2
Compounds Tested
2
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-V/beta-5 (CHEMBL2096675)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Profile of a Highly Selective Quaternized Pyrrolidine Betaine α<sub>v</sub>β<sub>6</sub> Integrin Inhibitor-(3<i>S</i>)-3-(3-(3,5-Dimethyl-1<i>H</i>-pyrazol-1-yl)phenyl)-4-((1<i>S</i> and 1<i>R</i>,3<i>R</i>)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation.
Barrett TN, Taylor JA, Barker D, Procopiou PA, Thompson JDF, Barrett J, Le J, Lynn SM, Pogany P, Pratley C, Pritchard JM, Roper JA, Rowedder JE, Slack RJ, Vitulli G, Macdonald SJF, Kerr WJ.
J Med Chem (2019) 62 : 7543 -7556
PubMed 31381331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.00 8.00
IC50 1 7.21 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4246089 GSK-3008348 1.0 1 8.00
CHEMBL3319237 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4246089 GSK-3008348 Ki = 10.0 nM 8.00
CHEMBL3319237 IC50 = 61.0 nM 7.21