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Assay Detail

CHEMBL617914

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

Binding
In vitro binding affinity at 5-hydroxytryptamine 2A receptor in rat cortical membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
Liégeois JF, Eyrolles L, Ellenbroek BA, Lejeune C, Carato P, Bruhwyler J, Géczy J, Damas J, Delarge J.
J Med Chem (2002) 45 : 5136 -5149
PubMed 12408724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.06 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148752 1 7.48
CHEMBL148694 1 7.47
CHEMBL148559 1 7.47
CHEMBL148353 1 7.44
CHEMBL422310 1 7.44
CHEMBL358657 1 7.32
CHEMBL342536 1 7.09
CHEMBL436274 1 6.99
CHEMBL356149 1 6.91
CHEMBL347959 1 6.88
CHEMBL149493 1 6.82
CHEMBL146410 1 6.60
CHEMBL356171 1 6.52
CHEMBL357391 1 6.45
CHEMBL355907 1 -
CHEMBL357325 1 -
CHEMBL148965 1 -
CHEMBL146856 1 -
CHEMBL347292 1 -
CHEMBL357743 1 -
CHEMBL148836 1 -
CHEMBL148952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148752 Ki = 33.0 nM 7.48
CHEMBL148694 Ki = 34.0 nM 7.47
CHEMBL148559 Ki = 34.0 nM 7.47
CHEMBL148353 Ki = 36.0 nM 7.44
CHEMBL422310 Ki = 36.0 nM 7.44
CHEMBL358657 Ki = 48.0 nM 7.32
CHEMBL342536 Ki = 81.0 nM 7.09
CHEMBL436274 Ki = 103.0 nM 6.99
CHEMBL356149 Ki = 123.0 nM 6.91
CHEMBL347959 Ki = 132.0 nM 6.88
CHEMBL149493 Ki = 150.0 nM 6.82
CHEMBL146410 Ki = 250.0 nM 6.60
CHEMBL356171 Ki = 303.0 nM 6.52
CHEMBL357391 Ki = 357.0 nM 6.45
CHEMBL355907 Ki > 1000.0 nM -
CHEMBL357325 Ki > 1000.0 nM -
CHEMBL148965 Ki > 1000.0 nM -
CHEMBL146856 Ki > 1000.0 nM -
CHEMBL347292 Ki > 1000.0 nM -
CHEMBL357743 Ki > 1000.0 nM -
CHEMBL148836 Ki > 1000.0 nM -
CHEMBL148952 Ki > 1000.0 nM -