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Assay Detail

CHEMBL754998

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

Binding
Ability to inhibit [3H]U-69593 binding to guinea pig Opioid receptor kappa 1
26
Total Activities
12
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

(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
Bertha CM, Vilner BJ, Mattson MV, Bowen WD, Becketts K, Xu H, Rothman RB, Flippen-Anderson JL, Rice KC.
J Med Chem (1995) 38 : 4776 -4785
PubMed 7490727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.13 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146659 3 6.61
CHEMBL38791 2 6.31
CHEMBL110319 3 6.24
CHEMBL141381 3 -
CHEMBL145296 3 -
CHEMBL322468 3 -
CHEMBL143800 3 -
CHEMBL109124 2 -
CHEMBL356639 1 -
CHEMBL358527 1 -
CHEMBL145422 1 -
CHEMBL145780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146659 Ki = 246.0 nM 6.61
CHEMBL38791 Ki = 491.0 nM 6.31
CHEMBL110319 Ki = 576.0 nM 6.24
CHEMBL110319 Ki = 889.0 nM 6.05
CHEMBL110319 Ki = 1091.0 nM 5.96
CHEMBL38791 Ki = 2536.0 nM 5.60
CHEMBL141381 Ki > 500.0 nM -
CHEMBL145296 Ki > 500.0 nM -
CHEMBL322468 Ki > 500.0 nM -
CHEMBL143800 Ki > 500.0 nM -
CHEMBL146659 Ki > 500.0 nM -
CHEMBL109124 Ki > 1000.0 nM -
CHEMBL146659 Ki > 500.0 nM -
CHEMBL109124 Ki > 500.0 nM -
CHEMBL322468 Ki > 500.0 nM -
CHEMBL141381 Ki > 500.0 nM -
CHEMBL358527 Ki > 500.0 nM -
CHEMBL141381 Ki > 500.0 nM -
CHEMBL322468 Ki > 500.0 nM -
CHEMBL143800 Ki > 500.0 nM -
CHEMBL145422 Ki > 1000.0 nM -
CHEMBL143800 Ki > 500.0 nM -
CHEMBL145296 Ki > 500.0 nM -
CHEMBL145780 Ki > 500.0 nM -
CHEMBL145296 Ki > 500.0 nM -
CHEMBL356639 Ki > 500.0 nM -