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Assay Detail

CHEMBL753278

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

Binding
Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE 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

Delta-type opioid receptor (CHEMBL269)
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 8.28 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20775 DELTORPHIN A 1 9.92
CHEMBL28401 1 9.70
CHEMBL282202 1 9.66
CHEMBL27253 1 9.66
CHEMBL340032 DADLE 1 9.59
CHEMBL435358 1 8.91
CHEMBL30066 1 8.51
CHEMBL26861 1 8.22
CHEMBL417837 1 8.22
CHEMBL282181 1 8.11
CHEMBL282139 1 8.06
CHEMBL287207 1 8.03
CHEMBL273820 1 7.97
CHEMBL278789 DERMORPHIN 1 6.87
CHEMBL26632 1 6.81
CHEMBL38874 DAMGO 1 6.74
CHEMBL28289 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20775 DELTORPHIN A Ki = 0.12 nM 9.92
CHEMBL28401 Ki = 0.2 nM 9.70
CHEMBL282202 Ki = 0.22 nM 9.66
CHEMBL27253 Ki = 0.22 nM 9.66
CHEMBL340032 DADLE Ki = 0.26 nM 9.59
CHEMBL435358 Ki = 1.23 nM 8.91
CHEMBL30066 Ki = 3.08 nM 8.51
CHEMBL26861 Ki = 6.01 nM 8.22
CHEMBL417837 Ki = 6.01 nM 8.22
CHEMBL282181 Ki = 7.71 nM 8.11
CHEMBL282139 Ki = 8.79 nM 8.06
CHEMBL287207 Ki = 9.42 nM 8.03
CHEMBL273820 Ki = 10.76 nM 7.97
CHEMBL278789 DERMORPHIN Ki = 134.0 nM 6.87
CHEMBL26632 Ki = 155.1 nM 6.81
CHEMBL38874 DAMGO Ki = 180.4 nM 6.74
CHEMBL28289 Ki = 1896.0 nM 5.72