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Assay Detail

CHEMBL617344

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Binding
Binding affinity was performed using [3H]ketanserin as the radioligand and stably transfected NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor (GF-62 cells).
19
Total Activities
19
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 (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
Runyon SP, Peddi S, Savage JE, Roth BL, Glennon RA, Westkaemper RB.
J Med Chem (2002) 45 : 1656 -1664
PubMed 11931619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.02 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47482 1 7.70
CHEMBL46566 1 7.19
CHEMBL44819 1 6.95
CHEMBL45207 1 6.71
CHEMBL44893 1 6.53
CHEMBL298271 1 6.48
CHEMBL46788 1 6.15
CHEMBL46979 1 6.11
CHEMBL297538 1 5.74
CHEMBL46449 1 5.64
CHEMBL46619 1 5.38
CHEMBL415906 1 5.35
CHEMBL10780 1 5.34
CHEMBL295814 1 5.17
CHEMBL42841 1 5.02
CHEMBL610 PHENETHYLAMINE 1 4.78
CHEMBL47983 1 -
CHEMBL45335 1 -
CHEMBL430935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47482 Ki = 20.0 nM 7.70
CHEMBL46566 Ki = 65.0 nM 7.19
CHEMBL44819 Ki = 112.0 nM 6.95
CHEMBL45207 Ki = 193.0 nM 6.71
CHEMBL44893 Ki = 296.0 nM 6.53
CHEMBL298271 Ki = 330.0 nM 6.48
CHEMBL46788 Ki = 711.0 nM 6.15
CHEMBL46979 Ki = 770.0 nM 6.11
CHEMBL297538 Ki = 1810.0 nM 5.74
CHEMBL46449 Ki = 2300.0 nM 5.64
CHEMBL46619 Ki = 4130.0 nM 5.38
CHEMBL415906 Ki = 4490.0 nM 5.35
CHEMBL10780 Ki = 4610.0 nM 5.34
CHEMBL295814 Ki = 6780.0 nM 5.17
CHEMBL42841 Ki = 9530.0 nM 5.02
CHEMBL610 PHENETHYLAMINE Ki = 16800.0 nM 4.78
CHEMBL47983 Ki > 10000.0 nM -
CHEMBL45335 Ki > 10000.0 nM -
CHEMBL430935 Ki > 10000.0 nM -