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Assay Detail

CHEMBL757986

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Binding
Compound was evaluated for binding affinity towards Opioid receptor mu 1 by displacement of [3H]-DAMGO radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.
Thomas JB, Atkinson RN, Rothman RB, Burgess JP, Mascarella SW, Dersch CM, Xu H, Carroll FI.
Bioorg Med Chem Lett (2000) 10 : 1281 -1284
PubMed 10866400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.82 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085002 1 6.16
CHEMBL3085003 1 5.96
CHEMBL13470 SNC-80 1 5.79
CHEMBL3085004 1 5.59
CHEMBL22650 1 5.58
CHEMBL280698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085002 Ki = 686.0 nM 6.16
CHEMBL3085003 Ki = 1105.0 nM 5.96
CHEMBL13470 SNC-80 Ki = 1614.0 nM 5.79
CHEMBL3085004 Ki = 2547.0 nM 5.59
CHEMBL22650 Ki = 2623.0 nM 5.58
CHEMBL280698 Ki > 3400.0 nM -