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Assay Detail

CHEMBL675868

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

Binding
In vitro ability to displace [3H]spiroperidol from rat dopamine receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.
Guérémy C, Audiau F, Uzan A, Le Fur G, Léger JM, Carpy A.
J Med Chem (1982) 25 : 1459 -1465
PubMed 7154006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.67 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.70
CHEMBL33022 1 8.30
CHEMBL71 CHLORPROMAZINE 4.0 1 7.85
CHEMBL289889 1 7.80
CHEMBL285682 1 7.80
CHEMBL36177 1 7.75
CHEMBL34250 1 7.70
CHEMBL32914 1 7.64
CHEMBL34245 1 7.50
CHEMBL413743 1 7.47
CHEMBL407641 MEZILAMINE 2.0 1 7.40
CHEMBL417146 1 7.36
CHEMBL35491 1 7.28
CHEMBL35287 1 7.14
CHEMBL34491 1 7.00
CHEMBL34874 1 6.93
CHEMBL35125 1 6.92
CHEMBL417676 1 6.85
CHEMBL288330 1 6.85
CHEMBL285690 1 6.73
CHEMBL42 CLOZAPINE 4.0 1 6.50
CHEMBL418221 1 6.42
CHEMBL32777 1 6.32
CHEMBL35502 1 6.19
CHEMBL286107 1 6.10
CHEMBL284956 1 6.00
CHEMBL32664 1 5.80
CHEMBL26 SULPIRIDE 3.0 1 5.80
CHEMBL34820 1 5.52
CHEMBL34246 IPROZILAMINE 2.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.0 nM 8.70
CHEMBL33022 Ki = 5.0 nM 8.30
CHEMBL71 CHLORPROMAZINE Ki = 14.0 nM 7.85
CHEMBL289889 Ki = 16.0 nM 7.80
CHEMBL285682 Ki = 16.0 nM 7.80
CHEMBL36177 Ki = 18.0 nM 7.75
CHEMBL34250 Ki = 20.0 nM 7.70
CHEMBL32914 Ki = 23.0 nM 7.64
CHEMBL34245 Ki = 32.0 nM 7.50
CHEMBL413743 Ki = 34.0 nM 7.47
CHEMBL407641 MEZILAMINE Ki = 40.0 nM 7.40
CHEMBL417146 Ki = 44.0 nM 7.36
CHEMBL35491 Ki = 52.0 nM 7.28
CHEMBL35287 Ki = 72.0 nM 7.14
CHEMBL34491 Ki = 100.0 nM 7.00
CHEMBL34874 Ki = 117.0 nM 6.93
CHEMBL35125 Ki = 120.0 nM 6.92
CHEMBL417676 Ki = 140.0 nM 6.85
CHEMBL288330 Ki = 140.0 nM 6.85
CHEMBL285690 Ki = 185.0 nM 6.73
CHEMBL42 CLOZAPINE Ki = 320.0 nM 6.50
CHEMBL418221 Ki = 385.0 nM 6.42
CHEMBL32777 Ki = 480.0 nM 6.32
CHEMBL35502 Ki = 640.0 nM 6.19
CHEMBL286107 Ki = 800.0 nM 6.10
CHEMBL284956 Ki = 1000.0 nM 6.00
CHEMBL32664 Ki = 1600.0 nM 5.80
CHEMBL26 SULPIRIDE Ki = 1600.0 nM 5.80
CHEMBL34820 Ki = 3000.0 nM 5.52
CHEMBL34246 IPROZILAMINE Ki = 8000.0 nM 5.10
CHEMBL287509 Ki = 20000.0 nM 4.70
CHEMBL35759 Ki = 22000.0 nM 4.66
CHEMBL32554 Ki = 40000.0 nM 4.40
CHEMBL36410 Ki = 40000.0 nM 4.40