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Assay Detail

CHEMBL747754

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Functional
Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAP
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
Thomas JB, Atkinson RN, Herault XM, Rothman RB, Mascarella SW, Dersch CM, Xu H, Horel RB, Carroll FI.
Bioorg Med Chem Lett (1999) 9 : 3347 -3350
PubMed 10612597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.65 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13470 SNC-80 1 6.17
CHEMBL440765 U-69593 1 5.67
CHEMBL102497 1 5.44
CHEMBL115730 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13470 SNC-80 Kd = 673.0 nM 6.17
CHEMBL440765 U-69593 Kd = 2142.0 nM 5.67
CHEMBL102497 Kd = 3604.0 nM 5.44
CHEMBL115730 Kd = 4667.0 nM 5.33