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Assay Detail

CHEMBL618897

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

Binding
Compound was evaluated for affinity towards cerebral 5-hydroxytryptamine 2A receptor in homogenate of caudate putamen tissue from rat brain
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Caudate-putamen
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.
Tamagnan G, Baldwin RM, Kula NS, Baldessarini RJ, Innis RB.
Bioorg Med Chem Lett (2000) 10 : 1113 -1115
PubMed 10843230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.62 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13632 1 8.07
CHEMBL62 SCH-23390 1 7.97
CHEMBL274577 Cyclopentadienyltricarbonylrheniumbenzazepine (2`-CPTR-SCH-23390) 1 7.76
CHEMBL13325 1 7.66
CHEMBL427996 Cyclopentadienyltricarbonylrheniumbenzazepine (3`-CPTR-SCH-23390) 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13632 Ki = 8.5 nM 8.07
CHEMBL62 SCH-23390 Ki = 10.8 nM 7.97
CHEMBL274577 Cyclopentadienyltricarbonylrheniumbenzazepine (2`-CPTR-SCH-23390) Ki = 17.3 nM 7.76
CHEMBL13325 Ki = 22.1 nM 7.66
CHEMBL427996 Cyclopentadienyltricarbonylrheniumbenzazepine (3`-CPTR-SCH-23390) Ki = 227.0 nM 6.64