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Assay Detail

CHEMBL757989

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

Binding
Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement.
17
Total Activities
17
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

Function of negative charge in the "address domain" of deltorphins.
Lazarus LH, Salvadori S, Santagada V, Tomatis R, Wilson WE.
J Med Chem (1991) 34 : 1350 -1355
PubMed 1849997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.63 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 9.18
CHEMBL278789 DERMORPHIN 1 9.15
CHEMBL340032 DADLE 1 8.09
CHEMBL282139 1 7.24
CHEMBL282202 1 6.93
CHEMBL287207 1 6.83
CHEMBL28401 1 6.82
CHEMBL27253 1 6.69
CHEMBL435358 1 6.56
CHEMBL20775 DELTORPHIN A 1 6.47
CHEMBL28289 1 5.80
CHEMBL26861 1 5.79
CHEMBL417837 1 5.68
CHEMBL273820 1 5.57
CHEMBL26632 1 5.49
CHEMBL30066 1 5.47
CHEMBL282181 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 0.66 nM 9.18
CHEMBL278789 DERMORPHIN Ki = 0.7 nM 9.15
CHEMBL340032 DADLE Ki = 8.16 nM 8.09
CHEMBL282139 Ki = 57.5 nM 7.24
CHEMBL282202 Ki = 118.6 nM 6.93
CHEMBL287207 Ki = 149.5 nM 6.83
CHEMBL28401 Ki = 152.8 nM 6.82
CHEMBL27253 Ki = 206.3 nM 6.69
CHEMBL435358 Ki = 275.5 nM 6.56
CHEMBL20775 DELTORPHIN A Ki = 335.9 nM 6.47
CHEMBL28289 Ki = 1571.0 nM 5.80
CHEMBL26861 Ki = 1640.0 nM 5.79
CHEMBL417837 Ki = 2094.0 nM 5.68
CHEMBL273820 Ki = 2687.0 nM 5.57
CHEMBL26632 Ki = 3221.0 nM 5.49
CHEMBL30066 Ki = 3408.0 nM 5.47
CHEMBL282181 Ki = 10571.0 nM 4.98