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Assay Detail

CHEMBL673628

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

Binding
Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrrole mannich bases as potential antipsychotic agents.
Scott MK, Martin GE, DiStefano DL, Fedde CL, Kukla MJ, Barrett DL, Baldy WJ, Elgin RJ, Kesslick JM, Mathiasen JR.
J Med Chem (1992) 35 : 552 -558
PubMed 1346653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 8.03 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.70
CHEMBL152311 1 9.35
CHEMBL346168 1 9.19
CHEMBL428175 RWJ-25730 1 9.10
CHEMBL153136 1 8.96
CHEMBL155506 1 8.85
CHEMBL434512 1 8.80
CHEMBL422 TRIFLUOPERAZINE 4.0 1 8.66
CHEMBL152458 1 8.64
CHEMBL348002 1 8.51
CHEMBL347782 1 8.48
CHEMBL345506 1 8.48
CHEMBL357286 1 8.34
CHEMBL347056 1 8.30
CHEMBL347334 1 8.17
CHEMBL152363 1 8.15
CHEMBL71 CHLORPROMAZINE 4.0 1 8.11
CHEMBL348241 1 8.03
CHEMBL152776 1 8.02
CHEMBL348014 1 7.89
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.69
CHEMBL153335 1 7.65
CHEMBL153451 1 7.45
CHEMBL152336 1 7.27
CHEMBL42 CLOZAPINE 4.0 1 7.27
CHEMBL153490 1 7.26
CHEMBL153219 1 7.18
CHEMBL152424 1 7.10
CHEMBL357532 1 7.00
CHEMBL151966 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.2 nM 9.70
CHEMBL152311 Ki = 0.45 nM 9.35
CHEMBL346168 Ki = 0.65 nM 9.19
CHEMBL428175 RWJ-25730 Ki = 0.8 nM 9.10
CHEMBL153136 Ki = 1.1 nM 8.96
CHEMBL155506 Ki = 1.4 nM 8.85
CHEMBL434512 Ki = 1.6 nM 8.80
CHEMBL422 TRIFLUOPERAZINE Ki = 2.2 nM 8.66
CHEMBL152458 Ki = 2.3 nM 8.64
CHEMBL348002 Ki = 3.1 nM 8.51
CHEMBL345506 Ki = 3.3 nM 8.48
CHEMBL347782 Ki = 3.3 nM 8.48
CHEMBL357286 Ki = 4.6 nM 8.34
CHEMBL347056 Ki = 5.0 nM 8.30
CHEMBL347334 Ki = 6.7 nM 8.17
CHEMBL152363 Ki = 7.0 nM 8.15
CHEMBL71 CHLORPROMAZINE Ki = 7.8 nM 8.11
CHEMBL348241 Ki = 9.3 nM 8.03
CHEMBL152776 Ki = 9.5 nM 8.02
CHEMBL348014 Ki = 12.8 nM 7.89
CHEMBL267044 LEVOSULPIRIDE Ki = 20.6 nM 7.69
CHEMBL153335 Ki = 22.5 nM 7.65
CHEMBL153451 Ki = 35.2 nM 7.45
CHEMBL152336 Ki = 53.7 nM 7.27
CHEMBL42 CLOZAPINE Ki = 53.6 nM 7.27
CHEMBL153490 Ki = 54.9 nM 7.26
CHEMBL153219 Ki = 65.5 nM 7.18
CHEMBL152424 Ki = 80.0 nM 7.10
CHEMBL357532 Ki = 101.0 nM 7.00
CHEMBL151966 Ki = 167.0 nM 6.78
CHEMBL49 BUSPIRONE Ki = 367.0 nM 6.43
CHEMBL152204 Ki = 1000.0 nM 6.00
CHEMBL152617 Ki > 1000.0 nM -
CHEMBL153161 Ki > 1000.0 nM -
CHEMBL9666 Ki > 1000.0 nM -
CHEMBL346881 Ki > 100.0 nM -
CHEMBL153263 Ki > 100.0 nM -
CHEMBL152867 Ki > 80.0 nM -
CHEMBL346459 Ki > 1000.0 nM -