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Assay Detail

CHEMBL754207

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

Binding
Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
Zimmerman DM, Cantrell BE, Swartzendruber JK, Jones ND, Mendelsohn LG, Leander JD, Nickander RC.
J Med Chem (1988) 31 : 555 -560
PubMed 2831363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.25 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359363 1 9.64
CHEMBL155216 2 9.02
CHEMBL56585 CYCLAZOCINE 2.0 1 8.92
CHEMBL153538 1 8.38
CHEMBL70 MORPHINE 4.0 1 8.24
CHEMBL415284 NALORPHINE 2.0 1 8.19
CHEMBL60542 (+)-PENTAZOCINE 1 8.16
CHEMBL150667 1 7.54
CHEMBL153661 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359363 Ki = 0.23 nM 9.64
CHEMBL155216 Ki = 0.96 nM 9.02
CHEMBL56585 CYCLAZOCINE Ki = 1.2 nM 8.92
CHEMBL153538 Ki = 4.2 nM 8.38
CHEMBL70 MORPHINE Ki = 5.7 nM 8.24
CHEMBL415284 NALORPHINE Ki = 6.5 nM 8.19
CHEMBL60542 (+)-PENTAZOCINE Ki = 6.9 nM 8.16
CHEMBL155216 Ki = 8.9 nM 8.05
CHEMBL150667 Ki = 29.0 nM 7.54
CHEMBL153661 Ki = 473.0 nM 6.33