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Assay Detail

CHEMBL675840

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

Binding
Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
Yevich JP, Temple DL, New JS, Taylor DP, Riblet LA.
J Med Chem (1983) 26 : 194 -203
PubMed 6131130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.73 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6066838 1 8.70
CHEMBL54 HALOPERIDOL 4.0 1 8.18
CHEMBL64348 1 7.30
CHEMBL27429 1 7.29
CHEMBL479 THIORIDAZINE 4.0 1 7.07
CHEMBL13647 BMY-7378 1 7.04
CHEMBL60322 1 7.04
CHEMBL64803 1 6.96
CHEMBL59638 1 6.96
CHEMBL292705 1 6.92
CHEMBL49 BUSPIRONE 4.0 1 6.92
CHEMBL305121 1 6.63
CHEMBL303810 1 6.54
CHEMBL62967 1 6.46
CHEMBL64084 1 6.41
CHEMBL296254 1 6.37
CHEMBL440302 1 6.37
CHEMBL292730 1 6.27
CHEMBL60733 1 6.24
CHEMBL62418 1 6.20
CHEMBL61330 1 6.19
CHEMBL64228 1 6.18
CHEMBL42 CLOZAPINE 4.0 1 6.05
CHEMBL302865 1 6.03
CHEMBL60154 1 6.02
CHEMBL293962 1 -
CHEMBL57364 1 -
CHEMBL61272 1 -
CHEMBL431750 1 -
CHEMBL293968 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6066838 IC50 = 2.0 nM 8.70
CHEMBL54 HALOPERIDOL IC50 = 6.6 nM 8.18
CHEMBL64348 IC50 = 50.0 nM 7.30
CHEMBL27429 IC50 = 51.0 nM 7.29
CHEMBL479 THIORIDAZINE IC50 = 85.0 nM 7.07
CHEMBL13647 BMY-7378 IC50 = 91.0 nM 7.04
CHEMBL60322 IC50 = 92.0 nM 7.04
CHEMBL64803 IC50 = 110.0 nM 6.96
CHEMBL59638 IC50 = 110.0 nM 6.96
CHEMBL49 BUSPIRONE IC50 = 120.0 nM 6.92
CHEMBL292705 IC50 = 120.0 nM 6.92
CHEMBL305121 IC50 = 236.0 nM 6.63
CHEMBL303810 IC50 = 290.0 nM 6.54
CHEMBL62967 IC50 = 350.0 nM 6.46
CHEMBL64084 IC50 = 390.0 nM 6.41
CHEMBL296254 IC50 = 430.0 nM 6.37
CHEMBL440302 IC50 = 430.0 nM 6.37
CHEMBL292730 IC50 = 540.0 nM 6.27
CHEMBL60733 IC50 = 570.0 nM 6.24
CHEMBL62418 IC50 = 630.0 nM 6.20
CHEMBL61330 IC50 = 640.0 nM 6.19
CHEMBL64228 IC50 = 660.0 nM 6.18
CHEMBL42 CLOZAPINE IC50 = 890.0 nM 6.05
CHEMBL302865 IC50 = 930.0 nM 6.03
CHEMBL60154 IC50 = 960.0 nM 6.02
CHEMBL60842 IC50 > 1000.0 nM -
CHEMBL303078 IC50 > 1000.0 nM -
CHEMBL58172 IC50 > 1000.0 nM -
CHEMBL27314 IC50 > 1000.0 nM -
CHEMBL284092 GEPIRONE IC50 > 1000.0 nM -
CHEMBL59643 IC50 > 1000.0 nM -
CHEMBL293968 IC50 > 1000.0 nM -
CHEMBL431750 IC50 > 1000.0 nM -
CHEMBL61272 IC50 > 1000.0 nM -
CHEMBL57364 IC50 > 1000.0 nM -
CHEMBL293962 IC50 > 1000.0 nM -