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Assay Detail

CHEMBL751990

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

Binding
Binding affinity at cloned human opioid receptor kappa 1
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Pagé D, Naismith A, Schmidt R, Coupal M, Labarre M, Gosselin M, Bellemare D, Payza K, Brown W.
J Med Chem (2001) 44 : 2387 -2390
PubMed 11448220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.70 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310842 1 8.89
CHEMBL76573 1 8.82
CHEMBL77001 1 8.82
CHEMBL421520 1 8.55
CHEMBL77804 1 8.39
CHEMBL80463 1 8.32
CHEMBL75802 1 7.29
CHEMBL76089 1 7.19
CHEMBL309307 1 6.51
CHEMBL309783 1 6.49
CHEMBL309236 1 6.46
CHEMBL307889 1 6.41
CHEMBL80197 1 6.28
CHEMBL77196 1 6.12
CHEMBL80464 1 6.10
CHEMBL310146 1 6.00
CHEMBL76846 1 5.97
CHEMBL80319 1 5.84
CHEMBL76493 1 5.60
CHEMBL312792 1 5.51
CHEMBL317956 DELTORPHIN C 1 5.13
CHEMBL80823 1 5.03
CHEMBL416788 1 4.43
CHEMBL308128 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310842 IC50 = 1.3 nM 8.89
CHEMBL76573 IC50 = 1.5 nM 8.82
CHEMBL77001 IC50 = 1.5 nM 8.82
CHEMBL421520 IC50 = 2.8 nM 8.55
CHEMBL77804 IC50 = 4.1 nM 8.39
CHEMBL80463 IC50 = 4.8 nM 8.32
CHEMBL75802 IC50 = 51.4 nM 7.29
CHEMBL76089 IC50 = 64.6 nM 7.19
CHEMBL309307 IC50 = 307.0 nM 6.51
CHEMBL309783 IC50 = 321.0 nM 6.49
CHEMBL309236 IC50 = 345.0 nM 6.46
CHEMBL307889 IC50 = 394.0 nM 6.41
CHEMBL80197 IC50 = 521.0 nM 6.28
CHEMBL77196 IC50 = 764.0 nM 6.12
CHEMBL80464 IC50 = 793.0 nM 6.10
CHEMBL310146 IC50 = 996.0 nM 6.00
CHEMBL76846 IC50 = 1070.0 nM 5.97
CHEMBL80319 IC50 = 1450.0 nM 5.84
CHEMBL76493 IC50 = 2510.0 nM 5.60
CHEMBL312792 IC50 = 3100.0 nM 5.51
CHEMBL317956 DELTORPHIN C IC50 = 7330.0 nM 5.13
CHEMBL80823 IC50 = 9380.0 nM 5.03
CHEMBL416788 IC50 = 37500.0 nM 4.43
CHEMBL308128 IC50 > 10000.0 nM -