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Assay Detail

CHEMBL4408647

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

Binding
Displacement of [3H]-DAMGO from full length human MOR expressed in chem5 cells incubated for 60 mins by liquid scintillation counter
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.
Lee H, Ahn S, Ann J, Ha H, Yoo YD, Kim YH, Hwang JY, Hur KH, Jang CG, Pearce LV, Esch TE, Lewin NE, Blumberg PM, Lee J.
Eur J Med Chem (2019) 182 : 111634 -111634
PubMed 31472474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.88 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 8.22
CHEMBL4457304 1 7.77
CHEMBL4438974 1 7.54
CHEMBL4536869 1 7.14
CHEMBL4476530 1 7.12
CHEMBL4448866 1 6.98
CHEMBL4471708 1 6.86
CHEMBL4459611 1 6.78
CHEMBL4453980 1 6.75
CHEMBL4442473 1 6.69
CHEMBL4457595 1 6.65
CHEMBL4562769 1 6.62
CHEMBL4555508 1 6.62
CHEMBL4438643 1 6.58
CHEMBL4571845 1 6.49
CHEMBL4483060 1 6.43
CHEMBL4586277 1 6.37
CHEMBL4553702 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE Ki = 6.08 nM 8.22
CHEMBL4457304 Ki = 17.0 nM 7.77
CHEMBL4438974 Ki = 29.0 nM 7.54
CHEMBL4536869 Ki = 72.4 nM 7.14
CHEMBL4476530 Ki = 76.2 nM 7.12
CHEMBL4448866 Ki = 105.0 nM 6.98
CHEMBL4471708 Ki = 137.0 nM 6.86
CHEMBL4459611 Ki = 166.0 nM 6.78
CHEMBL4453980 Ki = 177.0 nM 6.75
CHEMBL4442473 Ki = 205.0 nM 6.69
CHEMBL4457595 Ki = 225.0 nM 6.65
CHEMBL4562769 Ki = 240.0 nM 6.62
CHEMBL4555508 Ki = 240.0 nM 6.62
CHEMBL4438643 Ki = 261.0 nM 6.58
CHEMBL4571845 Ki = 322.0 nM 6.49
CHEMBL4483060 Ki = 368.0 nM 6.43
CHEMBL4586277 Ki = 428.0 nM 6.37
CHEMBL4553702 Ki = 507.0 nM 6.29