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Assay Detail

CHEMBL675094

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

Binding
In vitro inhibitory against radioligand [3H]spiperone binding to rat striatal Dopamine receptor D2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
Yevich JP, New JS, Lobeck WG, Dextraze P, Bernstein E, Taylor DP, Yocca FD, Eison MS, Temple DL.
J Med Chem (1992) 35 : 4516 -4525
PubMed 1361578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.90 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479 THIORIDAZINE 4.0 1 7.22
CHEMBL140831 1 6.70
CHEMBL141455 1 6.40
CHEMBL334934 1 6.38
CHEMBL140656 1 6.31
CHEMBL140872 1 6.17
CHEMBL137870 1 6.09
CHEMBL138186 1 6.03
CHEMBL335348 1 5.86
CHEMBL342484 1 5.77
CHEMBL443482 1 5.73
CHEMBL141226 1 5.73
CHEMBL141912 1 5.67
CHEMBL141922 1 5.66
CHEMBL141523 1 5.43
CHEMBL141854 1 5.41
CHEMBL139595 1 5.25
CHEMBL60859 BMY-14802 1 5.19
CHEMBL344577 1 5.06
CHEMBL140712 1 -
CHEMBL140833 1 -
CHEMBL137967 1 -
CHEMBL140650 1 -
CHEMBL141670 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479 THIORIDAZINE IC50 = 60.0 nM 7.22
CHEMBL140831 IC50 = 200.0 nM 6.70
CHEMBL141455 IC50 = 396.0 nM 6.40
CHEMBL334934 IC50 = 415.0 nM 6.38
CHEMBL140656 IC50 = 494.0 nM 6.31
CHEMBL140872 IC50 = 679.0 nM 6.17
CHEMBL137870 IC50 = 817.0 nM 6.09
CHEMBL138186 IC50 = 940.0 nM 6.03
CHEMBL335348 IC50 = 1380.0 nM 5.86
CHEMBL342484 IC50 = 1700.0 nM 5.77
CHEMBL443482 IC50 = 1880.0 nM 5.73
CHEMBL141226 IC50 = 1860.0 nM 5.73
CHEMBL141912 IC50 = 2120.0 nM 5.67
CHEMBL141922 IC50 = 2190.0 nM 5.66
CHEMBL141523 IC50 = 3750.0 nM 5.43
CHEMBL141854 IC50 = 3940.0 nM 5.41
CHEMBL139595 IC50 = 5660.0 nM 5.25
CHEMBL60859 BMY-14802 IC50 = 6430.0 nM 5.19
CHEMBL344577 IC50 = 8800.0 nM 5.06
CHEMBL140712 IC50 > 1000.0 nM -
CHEMBL140833 IC50 > 1000.0 nM -
CHEMBL137967 IC50 > 1000.0 nM -
CHEMBL140650 IC50 > 1000.0 nM -
CHEMBL141670 IC50 > 1000.0 nM -