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Assay Detail

CHEMBL4432235

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Functional
Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
Seltzman HH, Shiner C, Hirt EE, Gilliam AF, Thomas BF, Maitra R, Snyder R, Black SL, Patel PR, Mulpuri Y, Spigelman I.
J Med Chem (2016) 59 : 7525 -7543
PubMed 27482723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.77 6.98
Emax 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4516360 2 6.98
CHEMBL4483714 2 6.85
CHEMBL4443660 2 6.74
CHEMBL123515 2 6.71
CHEMBL127644 2 6.59
CHEMBL4438072 2 -
CHEMBL4519883 2 -
CHEMBL4435655 2 -
CHEMBL4550629 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4516360 EC50 = 104.0 nM 6.98
CHEMBL4483714 EC50 = 141.0 nM 6.85
CHEMBL4443660 EC50 = 182.0 nM 6.74
CHEMBL123515 EC50 = 196.0 nM 6.71
CHEMBL127644 EC50 = 257.0 nM 6.59
CHEMBL4519883 EC50 - -
CHEMBL4435655 EC50 - -
CHEMBL4550629 EC50 - -
CHEMBL4438072 EC50 - -
CHEMBL4519883 Emax - -
CHEMBL4435655 Emax - -
CHEMBL4516360 Emax = 79.0 % -
CHEMBL127644 Emax = 103.0 % -
CHEMBL123515 Emax = 114.0 % -
CHEMBL4550629 Emax - -
CHEMBL4483714 Emax = 121.0 % -
CHEMBL4443660 Emax = 108.0 % -
CHEMBL4438072 Emax - -