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Assay Detail

CHEMBL5253113

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

Binding
Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO-K1 cells incubated for 1 hr by 1450 microbeta scintillation counter analysis
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.
Brust A, Croker DE, Colless B, Ragnarsson L, Andersson Å, Jain K, Garcia-Caraballo S, Castro J, Brierley SM, Alewood PF, Lewis RJ.
J Med Chem (2016) 59 : 2381 -2395
PubMed 26859603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 79 7.66 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5273346 — — 1 10.15
CHEMBL5289754 — — 1 9.89
CHEMBL5281808 — — 1 9.80
CHEMBL5273114 — — 1 9.64
CHEMBL5281912 — — 1 9.60
CHEMBL5273273 — — 1 9.55
CHEMBL5286081 — — 1 9.54
CHEMBL415330 — — 1 9.40
CHEMBL5279208 — — 1 9.38
CHEMBL5282326 — — 1 9.32
CHEMBL5283811 — — 1 9.23
CHEMBL5278935 — — 1 9.23
CHEMBL5283035 — — 1 9.23
CHEMBL5288658 — — 1 9.21
CHEMBL5280997 — — 1 9.19
CHEMBL5284775 — — 1 9.15
CHEMBL5276702 — — 1 9.04
CHEMBL5285730 — — 1 9.01
CHEMBL5275165 — — 1 8.93
CHEMBL5270523 — — 1 8.92
CHEMBL5278992 — — 1 8.92
CHEMBL5282859 — — 1 8.92
CHEMBL5289642 — — 1 8.89
CHEMBL5280066 — — 1 8.89
CHEMBL5283084 — — 1 8.85
CHEMBL5276129 — — 1 8.68
CHEMBL5279518 — — 1 8.66
CHEMBL5288155 — — 1 8.62
CHEMBL5266718 — — 1 8.54
CHEMBL5268886 — — 1 8.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5273346 — Ki = 0.07 nM 10.15
CHEMBL5289754 — Ki = 0.13 nM 9.89
CHEMBL5281808 — Ki = 0.16 nM 9.80
CHEMBL5273114 — Ki = 0.23 nM 9.64
CHEMBL5281912 — Ki = 0.25 nM 9.60
CHEMBL5273273 — Ki = 0.28 nM 9.55
CHEMBL5286081 — Ki = 0.29 nM 9.54
CHEMBL415330 — Ki = 0.4 nM 9.40
CHEMBL5279208 — Ki = 0.42 nM 9.38
CHEMBL5282326 — Ki = 0.48 nM 9.32
CHEMBL5283811 — Ki = 0.59 nM 9.23
CHEMBL5278935 — Ki = 0.59 nM 9.23
CHEMBL5283035 — Ki = 0.59 nM 9.23
CHEMBL5288658 — Ki = 0.61 nM 9.21
CHEMBL5280997 — Ki = 0.64 nM 9.19
CHEMBL5284775 — Ki = 0.71 nM 9.15
CHEMBL5276702 — Ki = 0.91 nM 9.04
CHEMBL5285730 — Ki = 0.98 nM 9.01
CHEMBL5275165 — Ki = 1.18 nM 8.93
CHEMBL5270523 — Ki = 1.2 nM 8.92
CHEMBL5278992 — Ki = 1.2 nM 8.92
CHEMBL5282859 — Ki = 1.2 nM 8.92
CHEMBL5289642 — Ki = 1.3 nM 8.89
CHEMBL5280066 — Ki = 1.3 nM 8.89
CHEMBL5283084 — Ki = 1.4 nM 8.85
CHEMBL5276129 — Ki = 2.1 nM 8.68
CHEMBL5279518 — Ki = 2.2 nM 8.66
CHEMBL5288155 — Ki = 2.4 nM 8.62
CHEMBL5266718 — Ki = 2.9 nM 8.54
CHEMBL5268886 — Ki = 3.9 nM 8.41
CHEMBL5288478 — Ki = 5.3 nM 8.28
CHEMBL5280357 — Ki = 5.4 nM 8.27
CHEMBL5271178 — Ki = 6.7 nM 8.17
CHEMBL5267287 — Ki = 6.7 nM 8.17
CHEMBL5276505 — Ki = 7.8 nM 8.11
CHEMBL5276565 — Ki = 10.2 nM 7.99
CHEMBL5274492 — Ki = 13.0 nM 7.89
CHEMBL5288247 — Ki = 15.0 nM 7.82
CHEMBL5279099 — Ki = 15.8 nM 7.80
CHEMBL5268235 — Ki = 16.1 nM 7.79
CHEMBL5267374 — Ki = 19.4 nM 7.71
CHEMBL5284138 — Ki = 24.0 nM 7.62
CHEMBL5277937 — Ki = 28.0 nM 7.55
CHEMBL5271835 — Ki = 40.3 nM 7.39
CHEMBL5276375 — Ki = 60.0 nM 7.22
CHEMBL5281790 — Ki = 67.5 nM 7.17
CHEMBL5282726 — Ki = 80.0 nM 7.10
CHEMBL5269763 — Ki = 85.0 nM 7.07
CHEMBL5272472 — Ki = 133.0 nM 6.88
CHEMBL5265822 — Ki = 135.0 nM 6.87