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Assay Detail

CHEMBL758858

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Binding
Binding affinity against opioid receptor
2
Total Activities
2
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 (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Murali Dhar TG, Nagarathnam D, Marzabadi MR, Lagu B, Wong WC, Chiu G, Tyagarajan S, Miao SW, Zhang F, Sun W, Tian D, Shen Q, Zhang J, Wetzel JM, Forray C, Chang RS, Broten TP, Schorn TW, Chen TB, O'Malley S, Ransom R, Schneck K, Bendesky R, Harrell CM, Vyas KP.
J Med Chem (1999) 42 : 4778 -4793
PubMed 10579841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.15 4.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL357628 1 4.29
CHEMBL142243 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL357628 Ki = 51000.0 nM 4.29
CHEMBL142243 Ki = 100000.0 nM 4.00