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Assay Detail

CHEMBL617539

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

Binding
Binding affinity of [3H]ketanserin towards 5-hydroxytryptamine 2 receptor 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 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 7.79 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83915 1 8.68
CHEMBL42 CLOZAPINE 4.0 1 8.42
CHEMBL81330 1 8.24
CHEMBL309730 1 7.55
CHEMBL82591 1 7.52
CHEMBL71724 1 7.12
CHEMBL63329 1 7.03
CHEMBL69759 SONEPIPRAZOLE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83915 Ki = 2.1 nM 8.68
CHEMBL42 CLOZAPINE Ki = 3.8 nM 8.42
CHEMBL81330 Ki = 5.8 nM 8.24
CHEMBL309730 Ki = 28.0 nM 7.55
CHEMBL82591 Ki = 30.0 nM 7.52
CHEMBL71724 Ki = 76.0 nM 7.12
CHEMBL63329 Ki = 94.0 nM 7.03
CHEMBL69759 SONEPIPRAZOLE Ki > 1800.0 nM -