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Assay Detail

CHEMBL754613

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Binding
Binding affinity for kappa opioid receptor was measured using [3H]U-69593
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Ananthan S, Kezar HS, Saini SK, Khare NK, Davis P, Dersch CM, Porreca F, Rothman RB.
Bioorg Med Chem Lett (2003) 13 : 529 -532
PubMed 12565965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.83 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348011 1 9.15
CHEMBL149256 1 8.17
CHEMBL346173 1 8.06
CHEMBL357680 1 8.02
CHEMBL356387 1 7.92
CHEMBL346165 1 7.91
CHEMBL146907 1 7.72
CHEMBL150028 1 7.47
CHEMBL567175 NALTRINDOLE 1 7.45
CHEMBL356861 1 7.25
CHEMBL358208 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348011 Ki = 0.7 nM 9.15
CHEMBL149256 Ki = 6.7 nM 8.17
CHEMBL346173 Ki = 8.8 nM 8.06
CHEMBL357680 Ki = 9.6 nM 8.02
CHEMBL356387 Ki = 12.0 nM 7.92
CHEMBL346165 Ki = 12.2 nM 7.91
CHEMBL146907 Ki = 19.0 nM 7.72
CHEMBL150028 Ki = 33.9 nM 7.47
CHEMBL567175 NALTRINDOLE Ki = 35.8 nM 7.45
CHEMBL356861 Ki = 55.7 nM 7.25
CHEMBL358208 Ki = 92.0 nM 7.04