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Assay Detail

CHEMBL670448

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

Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
Campiani G, Butini S, Fattorusso C, Catalanotti B, Gemma S, Nacci V, Morelli E, Cagnotto A, Mereghetti I, Mennini T, Carli M, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Vertechy M, Di Serio S, Ghirardi O, Tinti O, Carminati P.
J Med Chem (2004) 47 : 143 -157
PubMed 14695828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.23 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303313 1 8.72
CHEMBL426763 1 8.72
CHEMBL64875 1 8.70
CHEMBL369367 1 8.47
CHEMBL177455 1 8.23
CHEMBL366679 1 8.11
CHEMBL368324 1 7.79
CHEMBL367045 1 7.71
CHEMBL176169 1 7.15
CHEMBL715 OLANZAPINE 4.0 1 7.07
CHEMBL54 HALOPERIDOL 4.0 1 6.50
CHEMBL42 CLOZAPINE 4.0 1 6.45
CHEMBL367087 1 5.79
CHEMBL367180 1 5.76
CHEMBL362060 1 5.37
CHEMBL367875 1 5.12
CHEMBL175226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303313 Ki = 1.9 nM 8.72
CHEMBL426763 Ki = 1.9 nM 8.72
CHEMBL64875 Ki = 2.0 nM 8.70
CHEMBL369367 Ki = 3.4 nM 8.47
CHEMBL177455 Ki = 5.87 nM 8.23
CHEMBL366679 Ki = 7.7 nM 8.11
CHEMBL368324 Ki = 16.4 nM 7.79
CHEMBL367045 Ki = 19.7 nM 7.71
CHEMBL176169 Ki = 71.0 nM 7.15
CHEMBL715 OLANZAPINE Ki = 85.0 nM 7.07
CHEMBL54 HALOPERIDOL Ki = 318.0 nM 6.50
CHEMBL42 CLOZAPINE Ki = 353.0 nM 6.45
CHEMBL367087 Ki = 1621.0 nM 5.79
CHEMBL367180 Ki = 1741.0 nM 5.76
CHEMBL362060 Ki = 4285.0 nM 5.37
CHEMBL367875 Ki = 7604.0 nM 5.12
CHEMBL175226 Ki > 1000000.0 nM -