Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL616887

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

Binding
Displacement of [3H]-ketanserin from human cloned 5-hydroxytryptamine 2A receptor expressed in CHO-K1 cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Some benzenesulfonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor
Weinhardt KK, Bonhaus DW, De Souza A
Bioorg Med Chem Lett (1996) 6 : 2687 -2692
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.30 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 8.80
CHEMBL12314 MESULERGINE 2.0 1 7.70
CHEMBL88402 RS-102,221 1 6.20
CHEMBL90175 1 6.10
CHEMBL88894 1 6.10
CHEMBL90565 1 6.00
CHEMBL91454 1 5.90
CHEMBL88193 1 5.70
CHEMBL90467 1 5.70
CHEMBL89967 1 5.60
CHEMBL88571 1 5.50
CHEMBL92809 1 -
CHEMBL328375 1 -
CHEMBL313745 1 -
CHEMBL88809 1 -
CHEMBL90267 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 1.585 nM 8.80
CHEMBL12314 MESULERGINE Ki = 19.95 nM 7.70
CHEMBL88402 RS-102,221 Ki = 630.96 nM 6.20
CHEMBL90175 Ki = 794.33 nM 6.10
CHEMBL88894 Ki = 794.33 nM 6.10
CHEMBL90565 Ki = 1000.0 nM 6.00
CHEMBL91454 Ki = 1258.93 nM 5.90
CHEMBL88193 Ki = 1995.26 nM 5.70
CHEMBL90467 Ki = 1995.26 nM 5.70
CHEMBL89967 Ki = 2511.89 nM 5.60
CHEMBL88571 Ki = 3162.28 nM 5.50
CHEMBL92809 Ki < 10000.0 nM -
CHEMBL328375 Ki < 10000.0 nM -
CHEMBL313745 Ki < 10000.0 nM -
CHEMBL88809 Ki < 10000.0 nM -
CHEMBL90267 Ki < 10000.0 nM -