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Assay Detail

CHEMBL2390779

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

Binding
Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis
24
Total Activities
24
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

Target

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

Publication

Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
Iyer MR, Rothman RB, Dersch CM, Jacobson AE, Rice KC.
Bioorg Med Chem (2013) 21 : 3298 -3309
PubMed 23618710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.49 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 8.92
CHEMBL70 MORPHINE 4.0 1 8.59
CHEMBL2386901 1 8.30
CHEMBL2386899 1 8.15
CHEMBL2386900 1 8.10
CHEMBL2386896 1 8.05
CHEMBL2386904 1 7.80
CHEMBL430441 1 7.72
CHEMBL2386898 1 7.66
CHEMBL2386902 1 7.64
CHEMBL2386823 1 7.55
CHEMBL2386822 1 7.35
CHEMBL2386897 1 7.31
CHEMBL2386819 1 7.22
CHEMBL2386820 1 7.18
CHEMBL2386891 1 7.08
CHEMBL2386893 1 7.04
CHEMBL2386895 1 7.02
CHEMBL2386892 1 7.01
CHEMBL2386894 1 6.78
CHEMBL2386821 1 6.78
CHEMBL2386903 1 6.76
CHEMBL2386824 1 6.37
CHEMBL440765 U-69593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 1.2 nM 8.92
CHEMBL70 MORPHINE Ki = 2.6 nM 8.59
CHEMBL2386901 Ki = 5.0 nM 8.30
CHEMBL2386899 Ki = 7.0 nM 8.15
CHEMBL2386900 Ki = 8.0 nM 8.10
CHEMBL2386896 Ki = 9.0 nM 8.05
CHEMBL2386904 Ki = 16.0 nM 7.80
CHEMBL430441 Ki = 19.0 nM 7.72
CHEMBL2386898 Ki = 22.0 nM 7.66
CHEMBL2386902 Ki = 23.0 nM 7.64
CHEMBL2386823 Ki = 28.0 nM 7.55
CHEMBL2386822 Ki = 45.0 nM 7.35
CHEMBL2386897 Ki = 49.0 nM 7.31
CHEMBL2386819 Ki = 60.0 nM 7.22
CHEMBL2386820 Ki = 66.0 nM 7.18
CHEMBL2386891 Ki = 84.0 nM 7.08
CHEMBL2386893 Ki = 91.0 nM 7.04
CHEMBL2386895 Ki = 96.0 nM 7.02
CHEMBL2386892 Ki = 97.0 nM 7.01
CHEMBL2386894 Ki = 166.0 nM 6.78
CHEMBL2386821 Ki = 165.0 nM 6.78
CHEMBL2386903 Ki = 174.0 nM 6.76
CHEMBL2386824 Ki = 425.0 nM 6.37
CHEMBL440765 U-69593 Ki > 2000.0 nM -