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Assay Detail

CHEMBL747875

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

Binding
Concentration required for 50% inhibition of [3H]DAGO binding to mu opioid receptor in crude rat brain homogenates
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays: Opioid peptides
Houghten RA, Dooley CT
Bioorg Med Chem Lett (1993) 3 : 405 -412
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.11 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2370697 1 7.55
CHEMBL334624 1 7.55
CHEMBL131788 1 7.52
CHEMBL132750 1 7.47
CHEMBL133774 1 7.47
CHEMBL131755 1 7.46
CHEMBL131814 1 7.46
CHEMBL337200 1 7.43
CHEMBL337119 1 7.41
CHEMBL133220 1 7.40
CHEMBL337201 1 7.39
CHEMBL336752 1 7.39
CHEMBL35838 [LEU5]ENKEPHALIN 1 7.39
CHEMBL130610 1 7.34
CHEMBL133278 1 7.24
CHEMBL132253 1 7.23
CHEMBL335072 1 7.22
CHEMBL334857 1 7.19
CHEMBL132776 1 7.19
CHEMBL132775 1 7.12
CHEMBL134023 1 7.11
CHEMBL133381 1 7.11
CHEMBL133268 1 7.10
CHEMBL130197 1 7.01
CHEMBL132743 1 6.97
CHEMBL340058 1 6.97
CHEMBL338961 1 6.95
CHEMBL264515 1 6.85
CHEMBL131638 1 6.80
CHEMBL134185 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2370697 IC50 = 28.0 nM 7.55
CHEMBL334624 IC50 = 28.0 nM 7.55
CHEMBL131788 IC50 = 30.0 nM 7.52
CHEMBL132750 IC50 = 34.0 nM 7.47
CHEMBL133774 IC50 = 34.0 nM 7.47
CHEMBL131755 IC50 = 35.0 nM 7.46
CHEMBL131814 IC50 = 35.0 nM 7.46
CHEMBL337200 IC50 = 37.0 nM 7.43
CHEMBL337119 IC50 = 39.0 nM 7.41
CHEMBL133220 IC50 = 40.0 nM 7.40
CHEMBL336752 IC50 = 41.0 nM 7.39
CHEMBL35838 [LEU5]ENKEPHALIN IC50 = 41.0 nM 7.39
CHEMBL337201 IC50 = 41.0 nM 7.39
CHEMBL130610 IC50 = 46.0 nM 7.34
CHEMBL133278 IC50 = 57.0 nM 7.24
CHEMBL132253 IC50 = 59.0 nM 7.23
CHEMBL335072 IC50 = 60.0 nM 7.22
CHEMBL334857 IC50 = 65.0 nM 7.19
CHEMBL132776 IC50 = 65.0 nM 7.19
CHEMBL132775 IC50 = 75.0 nM 7.12
CHEMBL133381 IC50 = 77.0 nM 7.11
CHEMBL134023 IC50 = 78.0 nM 7.11
CHEMBL133268 IC50 = 80.0 nM 7.10
CHEMBL130197 IC50 = 98.0 nM 7.01
CHEMBL132743 IC50 = 107.0 nM 6.97
CHEMBL340058 IC50 = 108.0 nM 6.97
CHEMBL338961 IC50 = 112.0 nM 6.95
CHEMBL264515 IC50 = 141.0 nM 6.85
CHEMBL131638 IC50 = 158.0 nM 6.80
CHEMBL134185 IC50 = 167.0 nM 6.78
CHEMBL132760 IC50 = 168.0 nM 6.78
CHEMBL132023 IC50 = 189.0 nM 6.72
CHEMBL134136 IC50 = 201.0 nM 6.70
CHEMBL339933 IC50 = 204.0 nM 6.69
CHEMBL335882 IC50 = 214.0 nM 6.67
CHEMBL262770 IC50 = 223.0 nM 6.65
CHEMBL336863 IC50 = 315.0 nM 6.50
CHEMBL132804 IC50 = 381.0 nM 6.42