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Assay Detail

CHEMBL753423

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

Binding
Binding affinity of compound was measured on Opioid receptor mu 1 by competitive inhibition of radioligand [3H]DAMGO using cloned receptors transiently expressed on COS-7 (monkey kidney) cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
Arttamangkul S, Ishmael JE, Murray TF, Grandy DK, DeLander GE, Kieffer BL, Aldrich JV.
J Med Chem (1997) 40 : 1211 -1218
PubMed 9111295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.56 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2370887 1 7.00
CHEMBL2370831 1 6.68
CHEMBL2370832 1 6.50
CHEMBL2370877 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2370887 Ki = 100.0 nM 7.00
CHEMBL2370831 Ki = 210.0 nM 6.68
CHEMBL2370832 Ki = 320.0 nM 6.50
CHEMBL2370877 Ki = 910.0 nM 6.04