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Assay Detail

CHEMBL671597

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

Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL3361)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.
TenBrink RE, Bergh CL, Duncan JN, Harris DW, Huff RM, Lahti RA, Lawson CF, Lutzke BS, Martin IJ, Rees SA, Schlachter SK, Sih JC, Smith MW.
J Med Chem (1996) 39 : 2435 -2437
PubMed 8691438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.95 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71724 1 8.85
CHEMBL309730 1 8.66
CHEMBL81330 1 8.52
CHEMBL69759 SONEPIPRAZOLE 2.0 1 8.14
CHEMBL63329 1 7.68
CHEMBL83915 1 7.62
CHEMBL82591 1 7.60
CHEMBL42 CLOZAPINE 4.0 1 7.50
CHEMBL81649 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71724 Ki = 1.4 nM 8.85
CHEMBL309730 Ki = 2.2 nM 8.66
CHEMBL81330 Ki = 3.0 nM 8.52
CHEMBL69759 SONEPIPRAZOLE Ki = 7.2 nM 8.14
CHEMBL63329 Ki = 21.0 nM 7.68
CHEMBL83915 Ki = 24.0 nM 7.62
CHEMBL82591 Ki = 25.0 nM 7.60
CHEMBL42 CLOZAPINE Ki = 32.0 nM 7.50
CHEMBL81649 Ki = 100.0 nM 7.00