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Assay Detail

CHEMBL831910

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Binding
Displacement of [3H]spiperone from dopamine D2 receptor of rat striatal membranes
ChEMBL ↗
46
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Heinrich T, Böttcher H, Gericke R, Bartoszyk GD, Anzali S, Seyfried CA, Greiner HE, Van Amsterdam C.
J Med Chem (2004) 47 : 4684 -4692
PubMed 15341484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.56 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427523 — — 1 9.15
CHEMBL359566 — — 1 8.85
CHEMBL433968 — — 1 8.85
CHEMBL188835 — — 1 8.42
CHEMBL188409 — — 1 8.38
CHEMBL188799 — — 1 8.31
CHEMBL189709 — — 1 8.25
CHEMBL189759 — — 1 8.24
CHEMBL185805 — — 1 8.22
CHEMBL188834 — — 1 8.18
CHEMBL184343 — — 1 8.10
CHEMBL185730 — — 1 8.03
CHEMBL185631 — — 1 7.89
CHEMBL186468 — — 1 7.55
CHEMBL189033 — — 1 7.51
CHEMBL186654 — — 1 7.46
CHEMBL188530 — — 1 7.41
CHEMBL184162 — — 1 7.40
CHEMBL364592 — — 1 7.40
CHEMBL363754 — — 1 7.37
CHEMBL189758 — — 1 7.34
CHEMBL189722 — — 1 7.33
CHEMBL363055 — — 1 7.11
CHEMBL439849 VILAZODONE 4.0 2 7.02
CHEMBL188296 — — 1 6.92
CHEMBL186655 — — 1 6.89
CHEMBL366300 — — 1 6.85
CHEMBL186138 — — 1 6.66
CHEMBL186424 — — 1 6.59
CHEMBL189704 — — 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427523 — IC50 = 0.7 nM 9.15
CHEMBL359566 — IC50 = 1.4 nM 8.85
CHEMBL433968 — IC50 = 1.4 nM 8.85
CHEMBL188835 — IC50 = 3.8 nM 8.42
CHEMBL188409 — IC50 = 4.2 nM 8.38
CHEMBL188799 — IC50 = 4.9 nM 8.31
CHEMBL189709 — IC50 = 5.6 nM 8.25
CHEMBL189759 — IC50 = 5.7 nM 8.24
CHEMBL185805 — IC50 = 6.0 nM 8.22
CHEMBL188834 — IC50 = 6.6 nM 8.18
CHEMBL184343 — IC50 = 8.0 nM 8.10
CHEMBL185730 — IC50 = 9.4 nM 8.03
CHEMBL185631 — IC50 = 13.0 nM 7.89
CHEMBL186468 — IC50 = 28.0 nM 7.55
CHEMBL189033 — IC50 = 31.0 nM 7.51
CHEMBL186654 — IC50 = 35.0 nM 7.46
CHEMBL188530 — IC50 = 39.0 nM 7.41
CHEMBL184162 — IC50 = 40.0 nM 7.40
CHEMBL364592 — IC50 = 40.0 nM 7.40
CHEMBL363754 — IC50 = 43.0 nM 7.37
CHEMBL189758 — IC50 = 46.0 nM 7.34
CHEMBL189722 — IC50 = 47.0 nM 7.33
CHEMBL363055 — IC50 = 77.0 nM 7.11
CHEMBL439849 VILAZODONE IC50 = 95.0 nM 7.02
CHEMBL188296 — IC50 = 120.0 nM 6.92
CHEMBL186655 — IC50 = 130.0 nM 6.89
CHEMBL366300 — IC50 = 140.0 nM 6.85
CHEMBL186138 — IC50 = 220.0 nM 6.66
CHEMBL186424 — IC50 = 255.0 nM 6.59
CHEMBL439849 VILAZODONE IC50 = 666.0 nM 6.18
CHEMBL189704 — IC50 = 740.0 nM 6.13
CHEMBL184171 — IC50 = 1400.0 nM 5.85
CHEMBL188848 — IC50 < 100.0 nM -
CHEMBL185768 — IC50 < 100.0 nM -
CHEMBL360407 — IC50 > 100.0 nM -
CHEMBL185807 — IC50 > 100.0 nM -
CHEMBL188798 — IC50 < 100.0 nM -
CHEMBL186219 — IC50 > 100.0 nM -
CHEMBL184556 — IC50 > 630.0 nM -
CHEMBL360390 — IC50 > 100.0 nM -
CHEMBL188833 — IC50 > 100.0 nM -
CHEMBL364610 — IC50 > 100.0 nM -
CHEMBL189869 — IC50 < 100.0 nM -
CHEMBL188481 — IC50 < 42.0 nM -
CHEMBL187909 — IC50 > 270.0 nM -
CHEMBL278471 — IC50 > 100.0 nM -