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Assay Detail

CHEMBL889154

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 acid-induced calcium influx
5
Total Activities
5
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: 1. Conformationally restricted analogues of trans-cinnamides.
Norman MH, Zhu J, Fotsch C, Bo Y, Chen N, Chakrabarti P, Doherty EM, Gavva NR, Nishimura N, Nixey T, Ognyanov VI, Rzasa RM, Stec M, Surapaneni S, Tamir R, Viswanadhan VN, Treanor JJ.
J Med Chem (2007) 50 : 3497 -3514
PubMed 17585749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.85 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226723 1 9.52
CHEMBL226724 1 8.38
CHEMBL226672 1 8.16
CHEMBL226671 1 6.60
CHEMBL227364 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226723 IC50 = 0.3 nM 9.52
CHEMBL226724 IC50 = 4.2 nM 8.38
CHEMBL226672 IC50 = 6.9 nM 8.16
CHEMBL226671 IC50 = 250.0 nM 6.60
CHEMBL227364 IC50 = 270.0 nM 6.57