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Assay Detail

CHEMBL2390777

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

Binding
Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis
23
Total Activities
23
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

Kappa-type opioid receptor (CHEMBL237)
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 23 6.26 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440765 U-69593 1 8.46
CHEMBL2386901 1 7.80
CHEMBL2386823 1 7.15
CHEMBL2386902 1 7.10
CHEMBL2386822 1 6.79
CHEMBL2386821 1 6.62
CHEMBL70 MORPHINE 4.0 1 6.52
CHEMBL2386904 1 6.27
CHEMBL2386897 1 6.17
CHEMBL2386898 1 6.14
CHEMBL2386896 1 6.14
CHEMBL2386899 1 6.08
CHEMBL2386893 1 6.01
CHEMBL2386891 1 5.78
CHEMBL2386903 1 5.72
CHEMBL2386892 1 5.72
CHEMBL2386895 1 5.65
CHEMBL2386900 1 5.61
CHEMBL2386894 1 5.54
CHEMBL2386819 1 5.54
CHEMBL2386820 1 5.45
CHEMBL2386824 1 5.38
CHEMBL430441 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440765 U-69593 Ki = 3.5 nM 8.46
CHEMBL2386901 Ki = 16.0 nM 7.80
CHEMBL2386823 Ki = 71.0 nM 7.15
CHEMBL2386902 Ki = 80.0 nM 7.10
CHEMBL2386822 Ki = 163.0 nM 6.79
CHEMBL2386821 Ki = 238.0 nM 6.62
CHEMBL70 MORPHINE Ki = 299.0 nM 6.52
CHEMBL2386904 Ki = 541.0 nM 6.27
CHEMBL2386897 Ki = 670.0 nM 6.17
CHEMBL2386898 Ki = 721.0 nM 6.14
CHEMBL2386896 Ki = 730.0 nM 6.14
CHEMBL2386899 Ki = 826.0 nM 6.08
CHEMBL2386893 Ki = 971.0 nM 6.01
CHEMBL2386891 Ki = 1651.0 nM 5.78
CHEMBL2386903 Ki = 1922.0 nM 5.72
CHEMBL2386892 Ki = 1913.0 nM 5.72
CHEMBL2386895 Ki = 2217.0 nM 5.65
CHEMBL2386900 Ki = 2459.0 nM 5.61
CHEMBL2386894 Ki = 2879.0 nM 5.54
CHEMBL2386819 Ki = 2882.0 nM 5.54
CHEMBL2386820 Ki = 3544.0 nM 5.45
CHEMBL2386824 Ki = 4182.0 nM 5.38
CHEMBL430441 Ki > 5000.0 nM -