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Assay Detail

CHEMBL863649

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Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL ↗
106
Total Activities
106
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Kolasa T, Matulenko MA, Hakeem AA, Patel MV, Mortell K, Bhatia P, Henry R, Nakane M, Hsieh GC, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino B, El Kouhen O, Marsh KC, Wetter JM, Moreland RB, Brioni JD, Stewart AO.
J Med Chem (2006) 49 : 5093 -5109
PubMed 16913699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 106 7.12 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212298 — — 1 8.64
CHEMBL215849 — — 1 8.38
CHEMBL214314 — — 1 8.36
CHEMBL215723 — — 1 8.31
CHEMBL45244 PD-168,077 — 1 8.08
CHEMBL214190 — — 1 8.05
CHEMBL209447 — — 1 8.02
CHEMBL212189 — — 1 7.92
CHEMBL212847 — — 1 7.88
CHEMBL427048 — — 1 7.87
CHEMBL212188 — — 1 7.77
CHEMBL213518 — — 1 7.76
CHEMBL215670 — — 1 7.75
CHEMBL213106 — — 1 7.72
CHEMBL214343 — — 1 7.71
CHEMBL438961 — — 1 7.70
CHEMBL214440 — — 1 7.69
CHEMBL385350 — — 1 7.66
CHEMBL441529 — — 1 7.65
CHEMBL385826 — — 1 7.62
CHEMBL214954 — — 1 7.62
CHEMBL385230 — — 1 7.60
CHEMBL212595 — — 1 7.58
CHEMBL212861 — — 1 7.56
CHEMBL211836 — — 1 7.56
CHEMBL212782 — — 1 7.54
CHEMBL212902 — — 1 7.51
CHEMBL377050 — — 1 7.50
CHEMBL212291 — — 1 7.48
CHEMBL376955 — — 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212298 — EC50 = 2.3 nM 8.64
CHEMBL215849 — EC50 = 4.2 nM 8.38
CHEMBL214314 — EC50 = 4.4 nM 8.36
CHEMBL215723 — EC50 = 4.9 nM 8.31
CHEMBL45244 PD-168,077 EC50 = 8.3 nM 8.08
CHEMBL214190 — EC50 = 8.9 nM 8.05
CHEMBL209447 — EC50 = 9.5 nM 8.02
CHEMBL212189 — EC50 = 11.9 nM 7.92
CHEMBL212847 — EC50 = 13.1 nM 7.88
CHEMBL427048 — EC50 = 13.6 nM 7.87
CHEMBL212188 — EC50 = 17.1 nM 7.77
CHEMBL213518 — EC50 = 17.5 nM 7.76
CHEMBL215670 — EC50 = 18.0 nM 7.75
CHEMBL213106 — EC50 = 19.2 nM 7.72
CHEMBL214343 — EC50 = 19.4 nM 7.71
CHEMBL438961 — EC50 = 20.0 nM 7.70
CHEMBL214440 — EC50 = 20.3 nM 7.69
CHEMBL385350 — EC50 = 21.7 nM 7.66
CHEMBL441529 — EC50 = 22.6 nM 7.65
CHEMBL385826 — EC50 = 24.1 nM 7.62
CHEMBL214954 — EC50 = 24.0 nM 7.62
CHEMBL385230 — EC50 = 25.0 nM 7.60
CHEMBL212595 — EC50 = 26.0 nM 7.58
CHEMBL212861 — EC50 = 27.6 nM 7.56
CHEMBL211836 — EC50 = 27.5 nM 7.56
CHEMBL212782 — EC50 = 28.5 nM 7.54
CHEMBL212902 — EC50 = 31.0 nM 7.51
CHEMBL377050 — EC50 = 32.0 nM 7.50
CHEMBL212291 — EC50 = 33.3 nM 7.48
CHEMBL376955 — EC50 = 33.0 nM 7.48
CHEMBL209645 — EC50 = 33.5 nM 7.47
CHEMBL212028 — EC50 = 34.5 nM 7.46
CHEMBL211732 — EC50 = 37.2 nM 7.43
CHEMBL212235 — EC50 = 37.6 nM 7.42
CHEMBL211972 — EC50 = 39.2 nM 7.41
CHEMBL213486 — EC50 = 40.1 nM 7.40
CHEMBL213828 — EC50 = 41.7 nM 7.38
CHEMBL212073 — EC50 = 42.3 nM 7.37
CHEMBL212891 — EC50 = 43.8 nM 7.36
CHEMBL211463 — EC50 = 44.8 nM 7.35
CHEMBL426510 — EC50 = 44.6 nM 7.35
CHEMBL213572 — EC50 = 45.0 nM 7.35
CHEMBL214247 — EC50 = 46.0 nM 7.34
CHEMBL211985 — EC50 = 45.8 nM 7.34
CHEMBL379546 — EC50 = 46.4 nM 7.33
CHEMBL215705 — EC50 = 46.7 nM 7.33
CHEMBL386867 — EC50 = 48.7 nM 7.31
CHEMBL212969 — EC50 = 48.8 nM 7.31
CHEMBL212545 — EC50 = 49.5 nM 7.30
CHEMBL212236 — EC50 = 56.6 nM 7.25