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Assay Detail

CHEMBL5360967

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

Binding
Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A systematic review on the kappa opioid receptor and its ligands: New directions for the treatment of pain, anxiety, depression, and drug abuse.
Khan MIH, Sawyer BJ, Akins NS, Le HV.
Eur J Med Chem (2022) 243 : 114785 -114785
PubMed 36179400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.01 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5431513 1 10.68
CHEMBL592 LEVORPHANOL 4.0 1 9.68
CHEMBL2368218 1 9.47
CHEMBL100116 PENTAZOCINE 4.0 1 8.49
CHEMBL60542 (+)-PENTAZOCINE 1 8.49
CHEMBL5401204 1 8.46
CHEMBL1186579 METHYLNALTREXONE 4.0 1 8.00
CHEMBL2180640 1 6.44
CHEMBL290543 1 6.43
CHEMBL5406584 1 6.27
CHEMBL4458783 1 5.72
CHEMBL5428706 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5431513 Ki = 0.021 nM 10.68
CHEMBL592 LEVORPHANOL Ki = 0.21 nM 9.68
CHEMBL2368218 Ki = 0.34 nM 9.47
CHEMBL100116 PENTAZOCINE Ki = 3.2 nM 8.49
CHEMBL60542 (+)-PENTAZOCINE Ki = 3.2 nM 8.49
CHEMBL5401204 Ki = 3.46 nM 8.46
CHEMBL1186579 METHYLNALTREXONE Ki = 10.0 nM 8.00
CHEMBL2180640 Ki = 360.0 nM 6.44
CHEMBL290543 Ki = 370.0 nM 6.43
CHEMBL5406584 Ki = 538.0 nM 6.27
CHEMBL4458783 Ki = 1900.0 nM 5.72
CHEMBL5428706 Ki > 10000.0 nM -