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Assay Detail

CHEMBL648042

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

Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 8.45 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.13
CHEMBL35057 TIOSPIRONE 2.0 1 8.82
CHEMBL37633 1 8.68
CHEMBL284847 1 8.64
CHEMBL35743 1 8.52
CHEMBL35085 1 8.38
CHEMBL287605 1 8.35
CHEMBL35565 1 8.29
CHEMBL42 CLOZAPINE 4.0 1 8.25
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL35040 1 8.19
CHEMBL708 ZIPRASIDONE 4.0 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.74 nM 9.13
CHEMBL35057 TIOSPIRONE Ki = 1.5 nM 8.82
CHEMBL37633 Ki = 2.1 nM 8.68
CHEMBL284847 Ki = 2.3 nM 8.64
CHEMBL35743 Ki = 3.0 nM 8.52
CHEMBL35085 Ki = 4.2 nM 8.38
CHEMBL287605 Ki = 4.5 nM 8.35
CHEMBL35565 Ki = 5.1 nM 8.29
CHEMBL42 CLOZAPINE Ki = 5.6 nM 8.25
CHEMBL54 HALOPERIDOL Ki = 6.3 nM 8.20
CHEMBL35040 Ki = 6.5 nM 8.19
CHEMBL708 ZIPRASIDONE Ki = 11.0 nM 7.96