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Assay Detail

CHEMBL5360966

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

Binding
Binding affinity to KOR (unknown origin) assessed as inhibition constant
14
Total Activities
14
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

Kappa-type opioid receptor (CHEMBL237)
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 14 8.76 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426627 1 10.10
CHEMBL5418013 1 9.62
CHEMBL440765 U-69593 1 9.52
CHEMBL5428706 1 9.49
CHEMBL2368218 1 9.38
CHEMBL592 LEVORPHANOL 4.0 1 8.64
CHEMBL4458783 1 8.62
CHEMBL5402380 1 8.60
CHEMBL5401204 1 8.46
CHEMBL100116 PENTAZOCINE 4.0 1 8.12
CHEMBL60542 (+)-PENTAZOCINE 1 8.12
CHEMBL2180640 1 7.96
CHEMBL5406584 1 7.30
CHEMBL5395105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426627 Ki = 0.08 nM 10.10
CHEMBL5418013 Ki = 0.24 nM 9.62
CHEMBL440765 U-69593 Ki = 0.3 nM 9.52
CHEMBL5428706 Ki = 0.32 nM 9.49
CHEMBL2368218 Ki = 0.42 nM 9.38
CHEMBL592 LEVORPHANOL Ki = 2.3 nM 8.64
CHEMBL4458783 Ki = 2.4 nM 8.62
CHEMBL5402380 Ki = 2.5 nM 8.60
CHEMBL5401204 Ki = 3.46 nM 8.46
CHEMBL100116 PENTAZOCINE Ki = 7.6 nM 8.12
CHEMBL60542 (+)-PENTAZOCINE Ki = 7.6 nM 8.12
CHEMBL2180640 Ki = 10.9 nM 7.96
CHEMBL5406584 Ki = 49.7 nM 7.30
CHEMBL5395105 Ki < 1.0 nM -