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Assay Detail

CHEMBL757824

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

Functional
Antagonistic activity against opioid receptor mu1
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Chen Z, Miller WS, Shan S, Valenzano KJ.
Bioorg Med Chem Lett (2003) 13 : 3247 -3252
PubMed 12951102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.57 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322515 1 9.00
CHEMBL325536 1 8.40
CHEMBL111230 1 8.10
CHEMBL112974 1 7.72
CHEMBL111347 1 7.68
CHEMBL111192 1 7.44
CHEMBL109563 1 7.34
CHEMBL113684 1 6.95
CHEMBL109598 1 6.91
CHEMBL320991 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322515 Ki = 1.0 nM 9.00
CHEMBL325536 Ki = 4.0 nM 8.40
CHEMBL111230 Ki = 8.0 nM 8.10
CHEMBL112974 Ki = 19.0 nM 7.72
CHEMBL111347 Ki = 21.0 nM 7.68
CHEMBL111192 Ki = 36.0 nM 7.44
CHEMBL109563 Ki = 46.0 nM 7.34
CHEMBL113684 Ki = 113.0 nM 6.95
CHEMBL109598 Ki = 124.0 nM 6.91
CHEMBL320991 Ki = 626.0 nM 6.20