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Assay Detail

CHEMBL5032712

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Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
35
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nociceptin receptor (CHEMBL2014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Mixed NOP/Opioid Receptor Peptide Agonists.
Pacifico S, Albanese V, Illuminati D, Marzola E, Fabbri M, Ferrari F, Holanda VAD, Sturaro C, Malfacini D, Ruzza C, Trapella C, Preti D, Lo Cascio E, Arcovito A, Della Longa S, Marangoni M, Fattori D, Nassini R, Calò G, Guerrini R.
J Med Chem (2021) 64 : 6656 -6669
PubMed 33998786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 7.72 9.29
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384755 1 9.29
CHEMBL429363 1 9.23
CHEMBL5073561 1 8.77
CHEMBL5070802 1 8.70
CHEMBL5093093 1 8.70
CHEMBL5080536 1 8.70
CHEMBL5074745 1 8.57
CHEMBL5081578 1 8.55
CHEMBL5079758 1 8.43
CHEMBL5081993 1 8.39
CHEMBL5092204 1 8.15
CHEMBL5085161 1 8.03
CHEMBL5086442 1 7.88
CHEMBL5093399 1 7.75
CHEMBL5070616 1 7.72
CHEMBL5094655 1 7.58
CHEMBL5094439 1 7.57
CHEMBL5081139 1 7.52
CHEMBL5070145 1 7.39
CHEMBL5090780 1 7.31
CHEMBL5072525 1 7.31
CHEMBL5073730 1 7.27
CHEMBL5086409 1 7.26
CHEMBL5092388 1 7.25
CHEMBL5072270 1 7.22
CHEMBL5075880 1 7.20
CHEMBL5081432 1 7.17
CHEMBL5081900 1 7.07
CHEMBL5079432 1 6.95
CHEMBL5078005 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384755 EC50 = 0.5129 nM 9.29
CHEMBL429363 EC50 = 0.5888 nM 9.23
CHEMBL5073561 EC50 = 1.698 nM 8.77
CHEMBL5070802 EC50 = 1.995 nM 8.70
CHEMBL5093093 EC50 = 1.995 nM 8.70
CHEMBL5080536 EC50 = 1.995 nM 8.70
CHEMBL5074745 EC50 = 2.692 nM 8.57
CHEMBL5081578 EC50 = 2.818 nM 8.55
CHEMBL5079758 EC50 = 3.715 nM 8.43
CHEMBL5081993 EC50 = 4.074 nM 8.39
CHEMBL5092204 EC50 = 7.079 nM 8.15
CHEMBL5085161 EC50 = 9.333 nM 8.03
CHEMBL5086442 EC50 = 13.18 nM 7.88
CHEMBL5093399 EC50 = 17.78 nM 7.75
CHEMBL5070616 EC50 = 19.05 nM 7.72
CHEMBL5094655 EC50 = 26.3 nM 7.58
CHEMBL5094439 EC50 = 26.92 nM 7.57
CHEMBL5081139 EC50 = 30.2 nM 7.52
CHEMBL5070145 EC50 = 40.74 nM 7.39
CHEMBL5090780 EC50 = 48.98 nM 7.31
CHEMBL5072525 EC50 = 48.98 nM 7.31
CHEMBL5073730 EC50 = 53.7 nM 7.27
CHEMBL5086409 EC50 = 54.95 nM 7.26
CHEMBL5092388 EC50 = 56.23 nM 7.25
CHEMBL5072270 EC50 = 60.26 nM 7.22
CHEMBL5075880 EC50 = 63.1 nM 7.20
CHEMBL5081432 EC50 = 67.61 nM 7.17
CHEMBL5081900 EC50 = 85.11 nM 7.07
CHEMBL5079432 EC50 = 112.2 nM 6.95
CHEMBL5078005 EC50 = 117.49 nM 6.93
CHEMBL5087383 EC50 = 123.03 nM 6.91
CHEMBL5081409 EC50 = 151.36 nM 6.82
CHEMBL5085090 EC50 = 245.47 nM 6.61
CHEMBL5091985 EC50 = 371.54 nM 6.43
CHEMBL285479 pEC50 - -