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Assay Detail

CHEMBL617265

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

Binding
Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor
12
Total Activities
12
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

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Howard HR, Lowe JA, Seeger TF, Seymour PA, Zorn SH, Maloney PR, Ewing FE, Newman ME, Schmidt AW, Furman JS, Robinson GL, Jackson E, Johnson C, Morrone J.
J Med Chem (1996) 39 : 143 -148
PubMed 8568801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 9.05 9.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35085 1 9.81
CHEMBL284847 1 9.57
CHEMBL35743 1 9.52
CHEMBL37633 1 9.48
CHEMBL35040 1 9.45
CHEMBL708 ZIPRASIDONE 4.0 1 9.38
CHEMBL85 RISPERIDONE 4.0 1 9.27
CHEMBL35057 TIOSPIRONE 2.0 1 9.24
CHEMBL35565 1 8.84
CHEMBL287605 1 8.84
CHEMBL42 CLOZAPINE 4.0 1 7.82
CHEMBL54 HALOPERIDOL 4.0 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35085 Ki = 0.1549 nM 9.81
CHEMBL284847 Ki = 0.2692 nM 9.57
CHEMBL35743 Ki = 0.302 nM 9.52
CHEMBL37633 Ki = 0.3311 nM 9.48
CHEMBL35040 Ki = 0.3548 nM 9.45
CHEMBL708 ZIPRASIDONE Ki = 0.4169 nM 9.38
CHEMBL85 RISPERIDONE Ki = 0.537 nM 9.27
CHEMBL35057 TIOSPIRONE Ki = 0.5754 nM 9.24
CHEMBL35565 Ki = 1.445 nM 8.84
CHEMBL287605 Ki = 1.445 nM 8.84
CHEMBL42 CLOZAPINE Ki = 15.14 nM 7.82
CHEMBL54 HALOPERIDOL Ki = 44.67 nM 7.35