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Assay Detail

CHEMBL1050690

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 cells
40
Total Activities
40
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 Intermediate

Target

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

Publication

Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Decker M, Si YG, Knapp BI, Bidlack JM, Neumeyer JL.
J Med Chem (2010) 53 : 402 -418
PubMed 19928862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 8.11 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571767 1 10.52
CHEMBL49269 CYCLORPHAN 1 10.47
CHEMBL568757 1 10.33
CHEMBL301160 BUTORPHAN 1 10.10
CHEMBL571998 1 9.47
CHEMBL568877 1 9.29
CHEMBL571990 1 9.23
CHEMBL570429 1 9.22
CHEMBL585901 1 9.21
CHEMBL568876 1 9.10
CHEMBL570654 1 9.00
CHEMBL570225 1 8.82
CHEMBL571561 1 8.80
CHEMBL571560 1 8.55
CHEMBL568988 1 8.41
CHEMBL569215 1 8.31
CHEMBL568989 1 8.28
CHEMBL576273 1 8.24
CHEMBL569725 1 7.92
CHEMBL571322 1 7.89
CHEMBL568813 1 7.80
CHEMBL572217 1 7.58
CHEMBL570428 1 7.58
CHEMBL572216 1 7.55
CHEMBL569009 1 7.52
CHEMBL568758 1 7.51
CHEMBL569313 1 7.43
CHEMBL569448 1 7.40
CHEMBL570449 1 7.40
CHEMBL568071 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571767 Ki = 0.03 nM 10.52
CHEMBL49269 CYCLORPHAN Ki = 0.034 nM 10.47
CHEMBL568757 Ki = 0.047 nM 10.33
CHEMBL301160 BUTORPHAN Ki = 0.079 nM 10.10
CHEMBL571998 Ki = 0.34 nM 9.47
CHEMBL568877 Ki = 0.51 nM 9.29
CHEMBL571990 Ki = 0.59 nM 9.23
CHEMBL570429 Ki = 0.6 nM 9.22
CHEMBL585901 Ki = 0.62 nM 9.21
CHEMBL568876 Ki = 0.79 nM 9.10
CHEMBL570654 Ki = 0.99 nM 9.00
CHEMBL570225 Ki = 1.5 nM 8.82
CHEMBL571561 Ki = 1.6 nM 8.80
CHEMBL571560 Ki = 2.8 nM 8.55
CHEMBL568988 Ki = 3.9 nM 8.41
CHEMBL569215 Ki = 4.9 nM 8.31
CHEMBL568989 Ki = 5.2 nM 8.28
CHEMBL576273 Ki = 5.8 nM 8.24
CHEMBL569725 Ki = 12.0 nM 7.92
CHEMBL571322 Ki = 13.0 nM 7.89
CHEMBL568813 Ki = 16.0 nM 7.80
CHEMBL570428 Ki = 26.0 nM 7.58
CHEMBL572217 Ki = 26.0 nM 7.58
CHEMBL572216 Ki = 28.0 nM 7.55
CHEMBL569009 Ki = 30.0 nM 7.52
CHEMBL568758 Ki = 31.0 nM 7.51
CHEMBL569313 Ki = 37.0 nM 7.43
CHEMBL569448 Ki = 40.0 nM 7.40
CHEMBL570449 Ki = 40.0 nM 7.40
CHEMBL568071 Ki = 44.0 nM 7.36
CHEMBL566128 Ki = 54.0 nM 7.27
CHEMBL567170 Ki = 67.0 nM 7.17
CHEMBL584530 Ki = 72.0 nM 7.14
CHEMBL568878 Ki = 86.0 nM 7.07
CHEMBL568830 Ki = 140.0 nM 6.85
CHEMBL569724 Ki = 280.0 nM 6.55
CHEMBL576065 Ki = 310.0 nM 6.51
CHEMBL568829 Ki = 340.0 nM 6.47
CHEMBL583265 Ki = 350.0 nM 6.46
CHEMBL578173 Ki = 380.0 nM 6.42