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Assay Detail

CHEMBL921652

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Functional
Agonist activity at kappa opioid receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.
Bioorg Med Chem Lett (2008) 18 : 3500 -3503
PubMed 18502123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.46 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255509 1 6.30
CHEMBL257767 1 6.10
CHEMBL402805 1 6.00
CHEMBL256937 1 6.00
CHEMBL255462 1 5.89
CHEMBL404289 1 5.89
CHEMBL256989 1 5.50
CHEMBL254356 1 5.50
CHEMBL257171 1 5.30
CHEMBL257150 1 5.30
CHEMBL258251 1 5.30
CHEMBL257415 1 5.20
CHEMBL402520 1 5.10
CHEMBL255460 1 5.10
CHEMBL402813 1 5.00
CHEMBL256988 1 4.82
CHEMBL256721 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255509 EC50 = 500.0 nM 6.30
CHEMBL257767 EC50 = 790.0 nM 6.10
CHEMBL402805 EC50 = 1000.0 nM 6.00
CHEMBL256937 EC50 = 1000.0 nM 6.00
CHEMBL255462 EC50 = 1300.0 nM 5.89
CHEMBL404289 EC50 = 1300.0 nM 5.89
CHEMBL256989 EC50 = 3200.0 nM 5.50
CHEMBL254356 EC50 = 3200.0 nM 5.50
CHEMBL257171 EC50 = 5000.0 nM 5.30
CHEMBL257150 EC50 = 5000.0 nM 5.30
CHEMBL258251 EC50 = 5000.0 nM 5.30
CHEMBL257415 EC50 = 6300.0 nM 5.20
CHEMBL402520 EC50 = 7900.0 nM 5.10
CHEMBL255460 EC50 = 7900.0 nM 5.10
CHEMBL402813 EC50 = 10000.0 nM 5.00
CHEMBL256988 EC50 = 15000.0 nM 4.82
CHEMBL256721 EC50 = 30000.0 nM 4.52