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Assay Detail

CHEMBL672949

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

Binding
Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone
55
Total Activities
55
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

Piperazinylalkyl heterocycles as potential antipsychotic agents.
Scott MK, Baxter EW, Bennett DJ, Boyd RE, Blum PS, Codd EE, Kukla MJ, Malloy E, Maryanoff BE, Maryanoff CA.
J Med Chem (1995) 38 : 4198 -4210
PubMed 7473547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 55 7.16 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.70
CHEMBL428175 RWJ-25730 1 8.92
CHEMBL10085 MAZAPERTINE 2.0 1 8.66
CHEMBL543900 1 8.52
CHEMBL133550 1 8.00
CHEMBL435198 1 8.00
CHEMBL543905 1 8.00
CHEMBL542483 1 7.62
CHEMBL1161061 1 7.58
CHEMBL544373 1 7.55
CHEMBL1161044 1 7.52
CHEMBL538280 1 7.52
CHEMBL1161071 1 7.48
CHEMBL1161074 1 7.30
CHEMBL1161065 1 7.30
CHEMBL42 CLOZAPINE 4.0 1 7.27
CHEMBL552830 1 7.17
CHEMBL1161067 1 7.14
CHEMBL1161063 1 7.09
CHEMBL1161072 1 7.00
CHEMBL1161068 1 7.00
CHEMBL1161057 1 7.00
CHEMBL1161051 1 7.00
CHEMBL1161075 1 7.00
CHEMBL1161055 1 7.00
CHEMBL1161054 1 6.91
CHEMBL1161060 1 6.89
CHEMBL1161095 1 6.78
CHEMBL1161094 1 6.52
CHEMBL1161073 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.2 nM 9.70
CHEMBL428175 RWJ-25730 Ki = 1.2 nM 8.92
CHEMBL10085 MAZAPERTINE Ki = 2.2 nM 8.66
CHEMBL543900 Ki = 3.0 nM 8.52
CHEMBL133550 Ki = 10.0 nM 8.00
CHEMBL435198 Ki = 10.0 nM 8.00
CHEMBL543905 Ki = 10.0 nM 8.00
CHEMBL542483 Ki = 24.0 nM 7.62
CHEMBL1161061 Ki = 26.0 nM 7.58
CHEMBL544373 Ki = 28.0 nM 7.55
CHEMBL1161044 Ki = 30.0 nM 7.52
CHEMBL538280 Ki = 30.0 nM 7.52
CHEMBL1161071 Ki = 33.0 nM 7.48
CHEMBL1161065 Ki = 50.0 nM 7.30
CHEMBL1161074 Ki = 50.0 nM 7.30
CHEMBL42 CLOZAPINE Ki = 53.6 nM 7.27
CHEMBL552830 Ki = 68.0 nM 7.17
CHEMBL1161067 Ki = 72.0 nM 7.14
CHEMBL1161063 Ki = 81.0 nM 7.09
CHEMBL1161072 Ki = 100.0 nM 7.00
CHEMBL1161068 Ki = 100.0 nM 7.00
CHEMBL1161057 Ki = 100.0 nM 7.00
CHEMBL1161051 Ki = 100.0 nM 7.00
CHEMBL1161075 Ki = 100.0 nM 7.00
CHEMBL1161055 Ki = 100.0 nM 7.00
CHEMBL1161054 Ki = 122.0 nM 6.91
CHEMBL1161060 Ki = 130.0 nM 6.89
CHEMBL1161095 Ki = 167.0 nM 6.78
CHEMBL1161094 Ki = 300.0 nM 6.52
CHEMBL1161073 Ki = 300.0 nM 6.52
CHEMBL1161064 Ki = 300.0 nM 6.52
CHEMBL1161052 Ki = 300.0 nM 6.52
CHEMBL1161097 Ki = 333.0 nM 6.48
CHEMBL49 BUSPIRONE Ki = 367.0 nM 6.43
CHEMBL1161069 Ki = 1000.0 nM 6.00
CHEMBL1161049 Ki = 1000.0 nM 6.00
CHEMBL1161043 Ki = 1431.0 nM 5.84
CHEMBL124285 Ki = 1841.0 nM 5.74
CHEMBL553555 Ki = 2415.0 nM 5.62
CHEMBL334889 Ki > 1000.0 nM -
CHEMBL1161053 Ki > 30.0 nM -
CHEMBL538529 Ki > 1000.0 nM -
CHEMBL1161062 Ki > 30.0 nM -
CHEMBL1161045 Ki > 1000.0 nM -
CHEMBL133880 Ki > 1000.0 nM -
CHEMBL1161070 Ki > 1000.0 nM -
CHEMBL1161048 Ki > 1000.0 nM -
CHEMBL544371 Ki > 1000.0 nM -
CHEMBL1161050 Ki > 1000.0 nM -
CHEMBL1161046 Ki > 1000.0 nM -