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Assay Detail

CHEMBL753955

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

Binding
Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes.
25
Total Activities
20
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

Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.
Lalinde N, Moliterni J, Wright D, Spencer HK, Ossipov MH, Spaulding TC, Rudo FG.
J Med Chem (1990) 33 : 2876 -2882
PubMed 2170652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.86 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327270 1 9.89
CHEMBL431047 1 9.82
CHEMBL319060 2 9.72
CHEMBL658 SUFENTANIL 4.0 1 9.66
CHEMBL95247 2 9.52
CHEMBL318958 2 9.48
CHEMBL95248 1 9.11
CHEMBL95909 1 8.96
CHEMBL95390 2 8.70
CHEMBL95786 1 8.70
CHEMBL70 MORPHINE 4.0 1 8.68
CHEMBL596 FENTANYL 4.0 1 8.67
CHEMBL319343 1 8.67
CHEMBL318895 1 8.55
CHEMBL100111 2 8.38
CHEMBL329950 1 8.12
CHEMBL634 ALFENTANIL 4.0 1 8.09
CHEMBL99596 1 8.09
CHEMBL317822 1 7.95
CHEMBL316670 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327270 Ki = 0.13 nM 9.89
CHEMBL431047 Ki = 0.15 nM 9.82
CHEMBL319060 Ki = 0.19 nM 9.72
CHEMBL658 SUFENTANIL Ki = 0.22 nM 9.66
CHEMBL95247 Ki = 0.3 nM 9.52
CHEMBL318958 Ki = 0.33 nM 9.48
CHEMBL95247 Ki = 0.4 nM 9.40
CHEMBL95248 Ki = 0.78 nM 9.11
CHEMBL318958 Ki = 0.86 nM 9.07
CHEMBL319060 Ki = 0.88 nM 9.06
CHEMBL95909 Ki = 1.1 nM 8.96
CHEMBL95786 Ki = 2.0 nM 8.70
CHEMBL95390 Ki = 2.0 nM 8.70
CHEMBL70 MORPHINE Ki = 2.1 nM 8.68
CHEMBL319343 Ki = 2.16 nM 8.67
CHEMBL596 FENTANYL Ki = 2.16 nM 8.67
CHEMBL318895 Ki = 2.8 nM 8.55
CHEMBL100111 Ki = 4.2 nM 8.38
CHEMBL329950 Ki = 7.62 nM 8.12
CHEMBL99596 Ki = 8.1 nM 8.09
CHEMBL634 ALFENTANIL Ki = 8.21 nM 8.09
CHEMBL317822 Ki = 11.2 nM 7.95
CHEMBL100111 Ki = 32.2 nM 7.49
CHEMBL316670 Ki > 100.0 nM -
CHEMBL95390 Ki > 1000.0 nM -