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Assay Detail

CHEMBL828927

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

Binding
Binding affinity against rat 5-hydroxytryptamine 2A receptor
7
Total Activities
7
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

4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Fish LR, Gilligan MT, Humphries AC, Ivarsson M, Ladduwahetty T, Merchant KJ, O'Connor D, Patel S, Philipps E, Vargas HM, Hutson PH, MacLeod AM.
Bioorg Med Chem Lett (2005) 15 : 3665 -3669
PubMed 15993598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.35 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74355 VOLINANSERIN 3.0 1 10.00
CHEMBL145939 1 9.74
CHEMBL176109 1 9.52
CHEMBL177807 1 9.29
CHEMBL175832 1 9.20
CHEMBL368816 1 8.88
CHEMBL178055 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74355 VOLINANSERIN Ki = 0.1 nM 10.00
CHEMBL145939 Ki = 0.18 nM 9.74
CHEMBL176109 Ki = 0.3 nM 9.52
CHEMBL177807 Ki = 0.51 nM 9.29
CHEMBL175832 Ki = 0.63 nM 9.20
CHEMBL368816 Ki = 1.33 nM 8.88
CHEMBL178055 Ki = 1.6 nM 8.80