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Assay Detail

CHEMBL675803

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

Binding
Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate
23
Total Activities
21
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

Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
Campiani G, Butini S, Gemma S, Nacci V, Fattorusso C, Catalanotti B, Giorgi G, Cagnotto A, Goegan M, Mennini T, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Ghirardi O, Tinti O, Carminati P.
J Med Chem (2002) 45 : 344 -359
PubMed 11784139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.92 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303313 1 9.40
CHEMBL64249 CLOROTEPINE 2.0 1 9.30
CHEMBL2111781 1 8.68
CHEMBL118889 1 8.51
CHEMBL121274 1 8.44
CHEMBL64875 1 8.44
CHEMBL120512 1 8.42
CHEMBL333955 1 8.40
CHEMBL54 HALOPERIDOL 4.0 1 8.32
CHEMBL116542 1 8.30
CHEMBL2111783 2 8.26
CHEMBL119687 1 8.22
CHEMBL333455 1 8.02
CHEMBL2111782 2 7.72
CHEMBL118919 1 7.66
CHEMBL332600 1 7.62
CHEMBL118092 1 7.52
CHEMBL368324 1 7.30
CHEMBL715 OLANZAPINE 4.0 1 7.16
CHEMBL333246 1 7.10
CHEMBL42 CLOZAPINE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303313 Ki = 0.4 nM 9.40
CHEMBL64249 CLOROTEPINE Ki = 0.5 nM 9.30
CHEMBL2111781 Ki = 2.1 nM 8.68
CHEMBL118889 Ki = 3.1 nM 8.51
CHEMBL121274 Ki = 3.6 nM 8.44
CHEMBL64875 Ki = 3.6 nM 8.44
CHEMBL120512 Ki = 3.8 nM 8.42
CHEMBL333955 Ki = 4.0 nM 8.40
CHEMBL54 HALOPERIDOL Ki = 4.8 nM 8.32
CHEMBL116542 Ki = 5.0 nM 8.30
CHEMBL2111783 Ki = 5.5 nM 8.26
CHEMBL119687 Ki = 6.0 nM 8.22
CHEMBL333455 Ki = 9.5 nM 8.02
CHEMBL2111782 Ki = 19.0 nM 7.72
CHEMBL118919 Ki = 22.0 nM 7.66
CHEMBL332600 Ki = 23.7 nM 7.62
CHEMBL118092 Ki = 30.0 nM 7.52
CHEMBL368324 Ki = 49.6 nM 7.30
CHEMBL715 OLANZAPINE Ki = 69.0 nM 7.16
CHEMBL333246 Ki = 79.0 nM 7.10
CHEMBL2111783 Ki = 245.0 nM 6.61
CHEMBL42 CLOZAPINE Ki = 250.0 nM 6.60
CHEMBL2111782 Ki = 601.0 nM 6.22