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Assay Detail

CHEMBL5031783

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Functional
Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay
ChEMBL ↗
42
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
Chakraborty S, DiBerto JF, Faouzi A, Bernhard SM, Gutridge AM, Ramsey S, Zhou Y, Provasi D, Nuthikattu N, Jilakara R, Nelson MNF, Asher WB, Eans SO, Wilson LL, Chintala SM, Filizola M, van Rijn RM, Margolis EB, Roth BL, McLaughlin JP, Che T, Sames D, Javitch JA, Majumdar S.
J Med Chem (2021) 64 : 13873 -13892
PubMed 34505767 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 7.01 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299031 — — 2 9.31
CHEMBL38874 DAMGO — 2 9.31
CHEMBL5074977 — — 2 8.28
CHEMBL61630 — — 2 8.23
CHEMBL5071286 — — 2 8.14
CHEMBL5081106 — — 2 7.95
CHEMBL5086376 — — 2 7.52
CHEMBL5086786 — — 2 7.44
CHEMBL5093673 — — 2 7.15
CHEMBL5075424 — — 2 7.08
CHEMBL5084960 — — 2 7.08
CHEMBL5094492 — — 2 7.07
CHEMBL5091787 — — 2 7.03
CHEMBL5075279 — — 2 6.98
CHEMBL5079202 — — 2 6.73
CHEMBL5075806 — — 2 6.43
CHEMBL5089366 — — 2 6.27
CHEMBL5093143 — — 2 5.95
CHEMBL5091971 — — 2 5.81
CHEMBL5088382 — — 2 5.42
CHEMBL5079626 — — 2 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO EC50 = 0.49 nM 9.31
CHEMBL299031 — EC50 = 0.4898 nM 9.31
CHEMBL5074977 — EC50 = 5.248 nM 8.28
CHEMBL5074977 — EC50 = 5.25 nM 8.28
CHEMBL38874 DAMGO EC50 = 5.888 nM 8.23
CHEMBL61630 — EC50 = 5.93 nM 8.23
CHEMBL5071286 — EC50 = 7.244 nM 8.14
CHEMBL5071286 — EC50 = 7.25 nM 8.14
CHEMBL5081106 — EC50 = 11.22 nM 7.95
CHEMBL5081106 — EC50 = 11.24 nM 7.95
CHEMBL5086376 — EC50 = 30.25 nM 7.52
CHEMBL5086376 — EC50 = 30.2 nM 7.52
CHEMBL5086786 — EC50 = 36.2 nM 7.44
CHEMBL5086786 — EC50 = 36.31 nM 7.44
CHEMBL5093673 — EC50 = 70.79 nM 7.15
CHEMBL5093673 — EC50 = 71.44 nM 7.15
CHEMBL5075424 — EC50 = 82.94 nM 7.08
CHEMBL5075424 — EC50 = 83.18 nM 7.08
CHEMBL5084960 — EC50 = 83.18 nM 7.08
CHEMBL5084960 — EC50 = 83.16 nM 7.08
CHEMBL5094492 — EC50 = 85.11 nM 7.07
CHEMBL5094492 — EC50 = 85.92 nM 7.07
CHEMBL5091787 — EC50 = 93.73 nM 7.03
CHEMBL5091787 — EC50 = 93.33 nM 7.03
CHEMBL5075279 — EC50 = 104.3 nM 6.98
CHEMBL5075279 — EC50 = 104.71 nM 6.98
CHEMBL5079202 — EC50 = 186.2 nM 6.73
CHEMBL5079202 — EC50 = 186.21 nM 6.73
CHEMBL299031 — EC50 = 241.2 nM 6.62
CHEMBL61630 — EC50 = 239.88 nM 6.62
CHEMBL5075806 — EC50 = 369.7 nM 6.43
CHEMBL5075806 — EC50 = 371.54 nM 6.43
CHEMBL5089366 — EC50 = 537.03 nM 6.27
CHEMBL5089366 — EC50 = 534.7 nM 6.27
CHEMBL5093143 — EC50 = 1122.02 nM 5.95
CHEMBL5093143 — EC50 = 1113.0 nM 5.95
CHEMBL5091971 — EC50 = 1548.82 nM 5.81
CHEMBL5091971 — EC50 = 1560.0 nM 5.81
CHEMBL5088382 — EC50 = 3801.89 nM 5.42
CHEMBL5088382 — EC50 = 3763.0 nM 5.42
CHEMBL5079626 — EC50 = 17510.0 nM 4.76
CHEMBL5079626 — EC50 = 17378.01 nM 4.76