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Assay Detail

CHEMBL755560

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

Binding
Binding affinity against opioid receptor mu in rats by displacing [3H]-DAGO
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.
Salvadori S, Bianchi C, Lazarus LH, Scaranari V, Attila M, Tomatis R.
J Med Chem (1992) 35 : 4651 -4657
PubMed 1335080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.01 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317956 DELTORPHIN C 1 6.57
CHEMBL342209 1 6.54
CHEMBL140384 1 6.30
CHEMBL263670 1 6.26
CHEMBL296603 DELTORPHINE II 1 6.20
CHEMBL142547 1 5.85
CHEMBL143354 1 5.84
CHEMBL143208 1 5.62
CHEMBL140845 1 5.61
CHEMBL139885 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317956 DELTORPHIN C Ki = 272.0 nM 6.57
CHEMBL342209 Ki = 287.0 nM 6.54
CHEMBL140384 Ki = 506.0 nM 6.30
CHEMBL263670 Ki = 554.0 nM 6.26
CHEMBL296603 DELTORPHINE II Ki = 638.0 nM 6.20
CHEMBL142547 Ki = 1413.0 nM 5.85
CHEMBL143354 Ki = 1429.0 nM 5.84
CHEMBL143208 Ki = 2391.0 nM 5.62
CHEMBL140845 Ki = 2460.0 nM 5.61
CHEMBL139885 Ki = 4787.0 nM 5.32