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Assay Detail

CHEMBL829674

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

Binding
Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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 relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
Costantino L, Gandolfi F, Sorbi C, Franchini S, Prezzavento O, Vittorio F, Ronsisvalle G, Leonardi A, Poggesi E, Brasili L.
J Med Chem (2005) 48 : 266 -273
PubMed 15634021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.89 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 9.38
CHEMBL54 HALOPERIDOL 4.0 1 8.57
CHEMBL1255588 1 8.44
CHEMBL85 RISPERIDONE 4.0 1 8.18
CHEMBL178700 1 6.35
CHEMBL179145 1 6.24
CHEMBL179371 1 6.06
CHEMBL178650 1 6.03
CHEMBL178519 1 5.96
CHEMBL434905 1 5.96
CHEMBL180327 1 5.94
CHEMBL179373 1 5.60
CHEMBL369133 1 -
CHEMBL179697 1 -
CHEMBL179808 1 -
CHEMBL276784 1 -
CHEMBL425867 1 -
CHEMBL360351 1 -
CHEMBL178924 1 -
CHEMBL178680 1 -
CHEMBL179530 1 -
CHEMBL180119 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 0.42 nM 9.38
CHEMBL54 HALOPERIDOL Ki = 2.69 nM 8.57
CHEMBL1255588 Ki = 3.61 nM 8.44
CHEMBL85 RISPERIDONE Ki = 6.65 nM 8.18
CHEMBL178700 Ki = 447.0 nM 6.35
CHEMBL179145 Ki = 575.0 nM 6.24
CHEMBL179371 Ki = 866.0 nM 6.06
CHEMBL178650 Ki = 924.0 nM 6.03
CHEMBL178519 Ki = 1093.0 nM 5.96
CHEMBL434905 Ki = 1093.0 nM 5.96
CHEMBL180327 Ki = 1145.0 nM 5.94
CHEMBL179373 Ki = 2493.0 nM 5.60
CHEMBL369133 Ki - nM -
CHEMBL179697 Ki > 1000.0 nM -
CHEMBL179808 Ki > 1000.0 nM -
CHEMBL276784 Ki > 1000.0 nM -
CHEMBL425867 Ki - nM -
CHEMBL360351 Ki - nM -
CHEMBL178924 Ki > 1000.0 nM -
CHEMBL178680 Ki > 1000.0 nM -
CHEMBL179530 Ki > 1000.0 nM -
CHEMBL180119 Ki > 1000.0 nM -