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Assay Detail

CHEMBL618692

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

Binding
Displacement of [3H]ketanserin from NIH3T3 cells stably expressing rat 5-hydroxytryptamine 2A receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
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 7.29 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108173 1 8.52
CHEMBL105292 1 8.40
CHEMBL102268 1 8.40
CHEMBL418994 1 8.10
CHEMBL105381 1 8.10
CHEMBL105580 1 7.92
CHEMBL292821 1 7.80
CHEMBL105152 1 7.77
CHEMBL104102 1 7.55
CHEMBL8334 1 7.52
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.50
CHEMBL103028 1 7.43
CHEMBL104088 1 7.22
CHEMBL101367 1 7.11
CHEMBL104715 1 7.02
CHEMBL439960 1 6.94
CHEMBL102274 1 6.82
CHEMBL104362 1 6.68
CHEMBL287047 1 5.52
CHEMBL280855 1 5.37
CHEMBL8642 1 5.33
CHEMBL16451 1 -
CHEMBL2367824 1 -
CHEMBL405 AMPHETAMINE 4.0 1 -
CHEMBL30577 1 -
CHEMBL16247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108173 Ki = 3.0 nM 8.52
CHEMBL105292 Ki = 4.0 nM 8.40
CHEMBL102268 Ki = 4.0 nM 8.40
CHEMBL418994 Ki = 8.0 nM 8.10
CHEMBL105381 Ki = 8.0 nM 8.10
CHEMBL105580 Ki = 12.0 nM 7.92
CHEMBL292821 Ki = 16.0 nM 7.80
CHEMBL105152 Ki = 17.0 nM 7.77
CHEMBL104102 Ki = 28.0 nM 7.55
CHEMBL8334 Ki = 30.0 nM 7.52
CHEMBL6607 BROLAMFETAMINE Ki = 32.0 nM 7.50
CHEMBL103028 Ki = 37.0 nM 7.43
CHEMBL104088 Ki = 60.0 nM 7.22
CHEMBL101367 Ki = 78.0 nM 7.11
CHEMBL104715 Ki = 95.0 nM 7.02
CHEMBL439960 Ki = 115.0 nM 6.94
CHEMBL102274 Ki = 150.0 nM 6.82
CHEMBL104362 Ki = 210.0 nM 6.68
CHEMBL287047 Ki = 3000.0 nM 5.52
CHEMBL280855 Ki = 4280.0 nM 5.37
CHEMBL8642 Ki = 4720.0 nM 5.33
CHEMBL16451 Ki > 10000.0 nM -
CHEMBL2367824 Ki > 10000.0 nM -
CHEMBL405 AMPHETAMINE Ki > 10000.0 nM -
CHEMBL30577 Ki > 10000.0 nM -
CHEMBL16247 Ki > 10000.0 nM -