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Assay Detail

CHEMBL890309

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

Functional
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R, Zhu J, Treanor JJ, Norman MH.
J Med Chem (2007) 50 : 3515 -3527
PubMed 17585750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.11 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229430 AMG-517 1.0 1 9.12
CHEMBL375681 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229430 AMG-517 IC50 = 0.76 nM 9.12
CHEMBL375681 IC50 = 0.8 nM 9.10