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Assay Detail

CHEMBL621512

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

Binding
Displacement of [3H]mesulergine from A9 cells stably expressing rat 5-hydroxytryptamine 2C receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.
Dowd CS, Herrick-Davis K, Egan C, DuPre A, Smith C, Teitler M, Glennon RA.
J Med Chem (2000) 43 : 3074 -3084
PubMed 10956215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.05 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418994 1 8.22
CHEMBL105580 1 7.80
CHEMBL104102 1 7.62
CHEMBL439960 1 7.60
CHEMBL102274 1 7.55
CHEMBL108173 1 7.41
CHEMBL102268 1 7.40
CHEMBL8334 1 7.30
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.19
CHEMBL103028 1 7.12
CHEMBL105292 1 7.10
CHEMBL105381 1 7.05
CHEMBL105152 1 6.87
CHEMBL104715 1 6.85
CHEMBL292821 1 6.72
CHEMBL104088 1 6.28
CHEMBL101367 1 6.28
CHEMBL104362 1 6.24
CHEMBL287047 1 5.26
CHEMBL16451 1 -
CHEMBL2367824 1 -
CHEMBL280855 1 -
CHEMBL8642 1 -
CHEMBL405 AMPHETAMINE 4.0 1 -
CHEMBL30577 1 -
CHEMBL16247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418994 Ki = 6.0 nM 8.22
CHEMBL105580 Ki = 16.0 nM 7.80
CHEMBL104102 Ki = 24.0 nM 7.62
CHEMBL439960 Ki = 25.0 nM 7.60
CHEMBL102274 Ki = 28.0 nM 7.55
CHEMBL108173 Ki = 39.0 nM 7.41
CHEMBL102268 Ki = 40.0 nM 7.40
CHEMBL8334 Ki = 50.0 nM 7.30
CHEMBL6607 BROLAMFETAMINE Ki = 64.0 nM 7.19
CHEMBL103028 Ki = 76.0 nM 7.12
CHEMBL105292 Ki = 79.0 nM 7.10
CHEMBL105381 Ki = 89.0 nM 7.05
CHEMBL105152 Ki = 135.0 nM 6.87
CHEMBL104715 Ki = 140.0 nM 6.85
CHEMBL292821 Ki = 190.0 nM 6.72
CHEMBL104088 Ki = 525.0 nM 6.28
CHEMBL101367 Ki = 530.0 nM 6.28
CHEMBL104362 Ki = 570.0 nM 6.24
CHEMBL287047 Ki = 5520.0 nM 5.26
CHEMBL16451 Ki > 10000.0 nM -
CHEMBL2367824 Ki > 10000.0 nM -
CHEMBL280855 Ki > 10000.0 nM -
CHEMBL8642 Ki > 10000.0 nM -
CHEMBL405 AMPHETAMINE Ki > 10000.0 nM -
CHEMBL30577 Ki > 10000.0 nM -
CHEMBL16247 Ki > 10000.0 nM -