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Assay Detail

CHEMBL670975

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
24
Total Activities
22
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 24 7.98 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303313 1 9.40
CHEMBL93240 METITEPINE 2.0 1 9.40
CHEMBL64249 CLOROTEPINE 2.0 1 9.30
CHEMBL2111781 1 8.69
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 8.23
CHEMBL333455 1 8.02
CHEMBL2111782 2 7.72
CHEMBL118919 1 7.66
CHEMBL332600 1 7.63
CHEMBL118092 1 7.53
CHEMBL368324 1 7.30
CHEMBL333246 1 7.10
CHEMBL715 OLANZAPINE 4.0 1 7.06
CHEMBL42 CLOZAPINE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE Ki = 0.3981 nM 9.40
CHEMBL303313 Ki = 0.3981 nM 9.40
CHEMBL64249 CLOROTEPINE Ki = 0.5012 nM 9.30
CHEMBL2111781 Ki = 2.042 nM 8.69
CHEMBL118889 Ki = 3.09 nM 8.51
CHEMBL121274 Ki = 3.631 nM 8.44
CHEMBL64875 Ki = 3.631 nM 8.44
CHEMBL120512 Ki = 3.802 nM 8.42
CHEMBL333955 Ki = 3.981 nM 8.40
CHEMBL54 HALOPERIDOL Ki = 4.786 nM 8.32
CHEMBL116542 Ki = 5.012 nM 8.30
CHEMBL2111783 Ki = 5.495 nM 8.26
CHEMBL119687 Ki = 5.888 nM 8.23
CHEMBL333455 Ki = 9.55 nM 8.02
CHEMBL2111782 Ki = 19.05 nM 7.72
CHEMBL118919 Ki = 21.88 nM 7.66
CHEMBL332600 Ki = 23.44 nM 7.63
CHEMBL118092 Ki = 29.51 nM 7.53
CHEMBL368324 Ki = 50.12 nM 7.30
CHEMBL333246 Ki = 79.43 nM 7.10
CHEMBL715 OLANZAPINE Ki = 87.1 nM 7.06
CHEMBL2111783 Ki = 245.47 nM 6.61
CHEMBL42 CLOZAPINE Ki = 251.19 nM 6.60
CHEMBL2111782 Ki = 602.56 nM 6.22