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Assay Detail

CHEMBL753956

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

Binding
Ability to inhibit [3H]DAMGO binding to rat brain Opioid receptor mu 1
26
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.78 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL145780 1 8.66
CHEMBL143800 3 8.41
CHEMBL322468 3 8.35
CHEMBL141381 3 8.19
CHEMBL38791 2 8.06
CHEMBL356639 1 8.04
CHEMBL358527 1 7.95
CHEMBL145296 3 7.93
CHEMBL146659 3 7.93
CHEMBL145422 1 7.57
CHEMBL110319 3 7.47
CHEMBL109124 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL145780 Ki = 2.2 nM 8.66
CHEMBL143800 Ki = 3.9 nM 8.41
CHEMBL143800 Ki = 4.1 nM 8.39
CHEMBL322468 Ki = 4.5 nM 8.35
CHEMBL322468 Ki = 6.1 nM 8.21
CHEMBL141381 Ki = 6.4 nM 8.19
CHEMBL38791 Ki = 8.7 nM 8.06
CHEMBL356639 Ki = 9.1 nM 8.04
CHEMBL358527 Ki = 11.2 nM 7.95
CHEMBL146659 Ki = 11.8 nM 7.93
CHEMBL145296 Ki = 11.8 nM 7.93
CHEMBL145296 Ki = 12.6 nM 7.90
CHEMBL141381 Ki = 21.6 nM 7.67
CHEMBL146659 Ki = 23.2 nM 7.63
CHEMBL145422 Ki = 26.7 nM 7.57
CHEMBL143800 Ki = 27.0 nM 7.57
CHEMBL145296 Ki = 31.4 nM 7.50
CHEMBL110319 Ki = 33.9 nM 7.47
CHEMBL38791 Ki = 35.5 nM 7.45
CHEMBL110319 Ki = 37.6 nM 7.42
CHEMBL322468 Ki = 45.1 nM 7.35
CHEMBL146659 Ki = 47.6 nM 7.32
CHEMBL141381 Ki = 48.2 nM 7.32
CHEMBL110319 Ki = 392.0 nM 6.41
CHEMBL109124 Ki > 250.0 nM -
CHEMBL109124 Ki > 250.0 nM -