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Assay Detail

CHEMBL617761

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

Binding
Displacement of [3H]mesulergine from human cloned 5-hydroxytryptamine 2C receptor expressed in CHO-K1 cells
23
Total Activities
23
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 2C (CHEMBL225)
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 23 8.04 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93862 1 9.70
CHEMBL91221 1 9.60
CHEMBL90565 1 8.80
CHEMBL91454 1 8.80
CHEMBL12314 MESULERGINE 2.0 1 8.70
CHEMBL88402 RS-102,221 1 8.70
CHEMBL310656 1 8.50
CHEMBL90346 1 8.40
CHEMBL88894 1 8.30
CHEMBL90470 1 8.20
CHEMBL90175 1 8.10
CHEMBL89967 1 8.00
CHEMBL328375 1 8.00
CHEMBL432217 1 8.00
CHEMBL90467 1 7.70
CHEMBL88571 1 7.50
CHEMBL88809 1 7.40
CHEMBL92809 1 7.40
CHEMBL88193 1 7.30
CHEMBL90267 1 7.10
CHEMBL313745 1 6.40
CHEMBL267930 SPIPERONE 2.0 1 6.20
CHEMBL90509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93862 Ki = 0.1995 nM 9.70
CHEMBL91221 Ki = 0.2512 nM 9.60
CHEMBL90565 Ki = 1.585 nM 8.80
CHEMBL91454 Ki = 1.585 nM 8.80
CHEMBL12314 MESULERGINE Ki = 1.995 nM 8.70
CHEMBL88402 RS-102,221 Ki = 1.995 nM 8.70
CHEMBL310656 Ki = 3.162 nM 8.50
CHEMBL90346 Ki = 3.981 nM 8.40
CHEMBL88894 Ki = 5.012 nM 8.30
CHEMBL90470 Ki = 6.31 nM 8.20
CHEMBL90175 Ki = 7.943 nM 8.10
CHEMBL89967 Ki = 10.0 nM 8.00
CHEMBL328375 Ki = 10.0 nM 8.00
CHEMBL432217 Ki = 10.0 nM 8.00
CHEMBL90467 Ki = 19.95 nM 7.70
CHEMBL88571 Ki = 31.62 nM 7.50
CHEMBL88809 Ki = 39.81 nM 7.40
CHEMBL92809 Ki = 39.81 nM 7.40
CHEMBL88193 Ki = 50.12 nM 7.30
CHEMBL90267 Ki = 79.43 nM 7.10
CHEMBL313745 Ki = 398.11 nM 6.40
CHEMBL267930 SPIPERONE Ki = 630.96 nM 6.20
CHEMBL90509 Ki < 10000.0 nM -