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Assay Detail

CHEMBL753771

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

Binding
Activity was evaluated by inhibition of the binding of 0.8 nM [3H]- DAMGO at Opioid receptor mu 1 binding site
19
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 (CHEMBL3041)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.
Schultz AG, Wang A, Alva C, Sebastian A, Glick SD, Deecher DC, Bidlack JM.
J Med Chem (1996) 39 : 1956 -1966
PubMed 8642554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.22 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 9.05
CHEMBL294226 3 8.70
CHEMBL431947 2 7.71
CHEMBL60270 1 7.56
CHEMBL409026 2 7.39
CHEMBL57879 2 7.38
CHEMBL58059 1 7.04
CHEMBL61644 1 6.99
CHEMBL418460 1 6.75
CHEMBL301421 2 6.53
CHEMBL299460 2 6.08
CHEMBL59840 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE Ki = 0.9 nM 9.05
CHEMBL294226 Ki = 1.99 nM 8.70
CHEMBL294226 Ki = 1.99 nM 8.70
CHEMBL294226 Ki = 2.29 nM 8.64
CHEMBL431947 Ki = 19.3 nM 7.71
CHEMBL431947 Ki = 25.2 nM 7.60
CHEMBL60270 Ki = 27.7 nM 7.56
CHEMBL409026 Ki = 40.6 nM 7.39
CHEMBL57879 Ki = 42.0 nM 7.38
CHEMBL409026 Ki = 41.2 nM 7.38
CHEMBL58059 Ki = 91.6 nM 7.04
CHEMBL61644 Ki = 102.0 nM 6.99
CHEMBL418460 Ki = 179.0 nM 6.75
CHEMBL301421 Ki = 297.0 nM 6.53
CHEMBL57879 Ki = 380.0 nM 6.42
CHEMBL299460 Ki = 830.0 nM 6.08
CHEMBL299460 Ki = 870.0 nM 6.06
CHEMBL301421 Ki = 2020.0 nM 5.70
CHEMBL59840 Ki = 3800.0 nM 5.42