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Assay Detail

CHEMBL675746

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

Binding
Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
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 8 6.33 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.26
CHEMBL81330 1 6.80
CHEMBL83915 1 6.40
CHEMBL63329 1 6.28
CHEMBL71724 1 5.96
CHEMBL81649 1 5.25
CHEMBL82591 1 -
CHEMBL69759 SONEPIPRAZOLE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 55.0 nM 7.26
CHEMBL81330 Ki = 160.0 nM 6.80
CHEMBL83915 Ki = 400.0 nM 6.40
CHEMBL63329 Ki = 530.0 nM 6.28
CHEMBL71724 Ki = 1100.0 nM 5.96
CHEMBL81649 Ki = 5600.0 nM 5.25
CHEMBL82591 Ki > 1800.0 nM -
CHEMBL69759 SONEPIPRAZOLE Ki > 4300.0 nM -