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Assay Detail

CHEMBL4775807

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Binding
Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of calcium uptake by 45Ca2+ uptake assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift.
Thorat SA,Lee Y,Jung A,Ann J,Ahn S,Baek J,Zuo D,Do N,Jeong JJ,Blumberg PM,Esch TE,Turcios NA,Pearce LV,Ha HJ,Yoo YD,Hong S,Choi S,Lee J
J Med Chem (2021) 64 : 370 -384
PubMed 33385210 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 7.58 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4789932 1 8.55
CHEMBL4789599 1 8.51
CHEMBL4787182 1 8.24
CHEMBL4776728 1 8.02
CHEMBL4800517 1 8.02
CHEMBL4785719 1 7.88
CHEMBL4797315 1 7.81
CHEMBL4776303 1 7.38
CHEMBL294199 CAPSAICIN 4.0 1 7.35
CHEMBL4798242 1 7.20
CHEMBL4789711 1 7.16
CHEMBL4800225 1 7.11
CHEMBL4782252 1 7.10
CHEMBL4792255 1 6.80
CHEMBL4779603 1 6.59
CHEMBL2177429 1 -
CHEMBL4781687 1 -
CHEMBL4783554 1 -
CHEMBL4790740 1 -
CHEMBL4794837 1 -
CHEMBL4782008 1 -
CHEMBL4786158 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4789932 EC50 = 2.79 nM 8.55
CHEMBL4789599 EC50 = 3.07 nM 8.51
CHEMBL4787182 EC50 = 5.81 nM 8.24
CHEMBL4776728 EC50 = 9.59 nM 8.02
CHEMBL4800517 EC50 = 9.59 nM 8.02
CHEMBL4785719 EC50 = 13.2 nM 7.88
CHEMBL4797315 EC50 = 15.5 nM 7.81
CHEMBL4776303 EC50 = 41.4 nM 7.38
CHEMBL294199 CAPSAICIN EC50 = 44.8 nM 7.35
CHEMBL4798242 EC50 = 63.2 nM 7.20
CHEMBL4789711 EC50 = 69.3 nM 7.16
CHEMBL4800225 EC50 = 78.6 nM 7.11
CHEMBL4782252 EC50 = 78.7 nM 7.10
CHEMBL4792255 EC50 = 160.0 nM 6.80
CHEMBL4779603 EC50 = 258.0 nM 6.59
CHEMBL2177429 EC50 - -
CHEMBL4781687 EC50 - -
CHEMBL4783554 EC50 - -
CHEMBL4790740 EC50 - -
CHEMBL4794837 EC50 - -
CHEMBL4782008 EC50 - -
CHEMBL4786158 EC50 - -