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Assay Detail

CHEMBL4236994

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

Binding
Antagonist activity at human integrin alphaVbeta6 in lung tissue slices derived from IPF patient assessed as reduction in SMAD2 phosphorylation
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.
Procopiou PA, Anderson NA, Barrett J, Barrett TN, Crawford MHJ, Fallon BJ, Hancock AP, Le J, Lemma S, Marshall RP, Morrell J, Pritchard JM, Rowedder JE, Saklatvala P, Slack RJ, Sollis SL, Suckling CJ, Thorp LR, Vitulli G, Macdonald SJF.
J Med Chem (2018) 61 : 8417 -8443
PubMed 30215258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 1 - -
IC50 1 9.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4241824 GSK-3008348 FREE BASE 1.0 2 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4241824 GSK-3008348 FREE BASE IC50 = 1.0 nM 9.00
CHEMBL4241824 GSK-3008348 FREE BASE Inhibition - % -