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Assay Detail

CHEMBL757520

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Binding
Binding affinity towards Opioid receptor mu 1 was determined in guinea pig whole brain using [3H]CTOP radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid receptors.
Boteju LW, Nikiforovich GV, Haskell-Luevano C, Fang SN, Zalewska T, Stropova D, Yamamura HI, Hruby VJ.
J Med Chem (1996) 39 : 4120 -4124
PubMed 8831778 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.50 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407057 1 6.16
CHEMBL2112688 1 5.52
CHEMBL2112689 1 5.17
CHEMBL31421 1 5.14
CHEMBL2111881 1 -
CHEMBL2111882 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407057 IC50 = 700.0 nM 6.16
CHEMBL2112688 IC50 = 3050.0 nM 5.52
CHEMBL2112689 IC50 = 6800.0 nM 5.17
CHEMBL31421 IC50 = 7300.0 nM 5.14
CHEMBL2111881 IC50 > 30000.0 nM -
CHEMBL2111882 IC50 > 30000.0 nM -