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Assay Detail

CHEMBL863653

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

Binding
Displacement of [3H]PIPAT from human recombinant D2L receptor expressed in HEK293 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
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
Ki 30 6.84 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437532 1 7.71
CHEMBL210101 1 7.60
CHEMBL213164 1 7.33
CHEMBL215450 1 7.21
CHEMBL212235 1 7.20
CHEMBL378324 1 7.19
CHEMBL212861 1 7.17
CHEMBL212903 1 7.17
CHEMBL212292 1 7.12
CHEMBL212784 1 7.01
CHEMBL426510 1 7.00
CHEMBL437687 1 6.95
CHEMBL211836 1 6.90
CHEMBL212782 1 6.89
CHEMBL211732 1 6.88
CHEMBL212444 1 6.86
CHEMBL376955 1 6.85
CHEMBL213004 1 6.84
CHEMBL212288 1 6.79
CHEMBL212969 1 6.78
CHEMBL378576 1 6.77
CHEMBL377050 1 6.76
CHEMBL427048 1 6.66
CHEMBL215705 1 6.65
CHEMBL377388 1 6.59
CHEMBL214314 1 6.59
CHEMBL441529 1 6.43
CHEMBL214247 1 6.00
CHEMBL212291 1 5.74
CHEMBL212891 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437532 Ki = 19.4 nM 7.71
CHEMBL210101 Ki = 25.3 nM 7.60
CHEMBL213164 Ki = 46.6 nM 7.33
CHEMBL215450 Ki = 60.9 nM 7.21
CHEMBL212235 Ki = 63.8 nM 7.20
CHEMBL378324 Ki = 64.5 nM 7.19
CHEMBL212861 Ki = 68.4 nM 7.17
CHEMBL212903 Ki = 68.0 nM 7.17
CHEMBL212292 Ki = 76.5 nM 7.12
CHEMBL212784 Ki = 98.7 nM 7.01
CHEMBL426510 Ki = 101.0 nM 7.00
CHEMBL437687 Ki = 112.0 nM 6.95
CHEMBL211836 Ki = 125.0 nM 6.90
CHEMBL212782 Ki = 128.0 nM 6.89
CHEMBL211732 Ki = 132.0 nM 6.88
CHEMBL212444 Ki = 137.0 nM 6.86
CHEMBL376955 Ki = 140.0 nM 6.85
CHEMBL213004 Ki = 146.0 nM 6.84
CHEMBL212288 Ki = 164.0 nM 6.79
CHEMBL212969 Ki = 168.0 nM 6.78
CHEMBL378576 Ki = 171.0 nM 6.77
CHEMBL377050 Ki = 172.0 nM 6.76
CHEMBL427048 Ki = 221.0 nM 6.66
CHEMBL215705 Ki = 225.0 nM 6.65
CHEMBL377388 Ki = 257.0 nM 6.59
CHEMBL214314 Ki = 257.0 nM 6.59
CHEMBL441529 Ki = 368.0 nM 6.43
CHEMBL214247 Ki = 995.0 nM 6.00
CHEMBL212291 Ki = 1820.0 nM 5.74
CHEMBL212891 Ki = 2530.0 nM 5.60