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Assay Detail

CHEMBL853453

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

Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nociceptin receptor (CHEMBL5492)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
Crooks PA, Kottayil SG, Al-Ghananeem AM, Byrn SR, Butterfield DA.
Bioorg Med Chem Lett (2006) 16 : 4291 -4295
PubMed 16777416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.02 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378753 1 9.52
CHEMBL214040 1 8.26
CHEMBL1418 1 8.20
CHEMBL385448 1 8.15
CHEMBL213228 1 7.95
CHEMBL70 MORPHINE 4.0 1 7.86
CHEMBL385048 1 7.70
CHEMBL38874 DAMGO 1 7.57
CHEMBL211576 1 6.58
CHEMBL13786 1 6.56
CHEMBL379928 1 6.40
CHEMBL1417 1 6.34
CHEMBL209751 1 6.29
CHEMBL1416 1 6.12
CHEMBL437682 1 6.08
CHEMBL213737 1 6.08
CHEMBL143939 1 5.99
CHEMBL440765 U-69593 1 5.96
CHEMBL1415 1 5.77
CHEMBL211374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378753 Ki = 0.3 nM 9.52
CHEMBL214040 Ki = 5.5 nM 8.26
CHEMBL1418 Ki = 6.3 nM 8.20
CHEMBL385448 Ki = 7.0 nM 8.15
CHEMBL213228 Ki = 11.2 nM 7.95
CHEMBL70 MORPHINE Ki = 13.9 nM 7.86
CHEMBL385048 Ki = 19.9 nM 7.70
CHEMBL38874 DAMGO Ki = 26.9 nM 7.57
CHEMBL211576 Ki = 266.0 nM 6.58
CHEMBL13786 Ki = 277.0 nM 6.56
CHEMBL379928 Ki = 400.0 nM 6.40
CHEMBL1417 Ki = 455.0 nM 6.34
CHEMBL209751 Ki = 513.0 nM 6.29
CHEMBL1416 Ki = 760.0 nM 6.12
CHEMBL437682 Ki = 838.0 nM 6.08
CHEMBL213737 Ki = 822.0 nM 6.08
CHEMBL143939 Ki = 1028.0 nM 5.99
CHEMBL440765 U-69593 Ki = 1099.0 nM 5.96
CHEMBL1415 Ki = 1694.0 nM 5.77
CHEMBL211374 Ki > 10000.0 nM -