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Assay Detail

CHEMBL671505

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

Binding
Binding affinity towards dopamine receptor D2 using as [3H]-spiperone radioligand.
16
Total Activities
16
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

Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2- pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydrobenzofuran-7-carboxamides.
Murakami S, Marubayashi N, Fukuda T, Takehara S, Tahara T.
J Med Chem (1991) 34 : 261 -267
PubMed 1825115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.01 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2114234 1 8.17
CHEMBL2114236 1 8.03
CHEMBL2115231 1 8.02
CHEMBL2115232 1 7.68
CHEMBL2114235 1 7.64
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.54
CHEMBL22857 1 7.29
CHEMBL2114240 1 7.23
CHEMBL2115229 1 7.02
CHEMBL2115228 1 6.68
CHEMBL278762 1 6.64
CHEMBL2114238 1 6.40
CHEMBL2115227 1 6.20
CHEMBL2114239 1 6.19
CHEMBL2115233 1 5.85
CHEMBL196677 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2114234 Ki = 6.7 nM 8.17
CHEMBL2114236 Ki = 9.4 nM 8.03
CHEMBL2115231 Ki = 9.6 nM 8.02
CHEMBL2115232 Ki = 21.0 nM 7.68
CHEMBL2114235 Ki = 23.0 nM 7.64
CHEMBL267044 LEVOSULPIRIDE Ki = 29.0 nM 7.54
CHEMBL22857 Ki = 51.0 nM 7.29
CHEMBL2114240 Ki = 59.0 nM 7.23
CHEMBL2115229 Ki = 95.0 nM 7.02
CHEMBL2115228 Ki = 210.0 nM 6.68
CHEMBL278762 Ki = 230.0 nM 6.64
CHEMBL2114238 Ki = 400.0 nM 6.40
CHEMBL2115227 Ki = 630.0 nM 6.20
CHEMBL2114239 Ki = 650.0 nM 6.19
CHEMBL2115233 Ki = 1400.0 nM 5.85
CHEMBL196677 Ki = 2700.0 nM 5.57