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Assay Detail

CHEMBL617522

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Binding
Displacement of [3H]ketanserin from human 5-hydroxytryptamine 2A receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.
Chang-Fong J, Addo J, Dukat M, Smith C, Mitchell NA, Herrick-Davis K, Teitler M, Glennon RA.
Bioorg Med Chem Lett (2002) 12 : 155 -158
PubMed 11755343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.08 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290779 1 7.24
CHEMBL289061 1 6.89
CHEMBL38633 1 6.22
CHEMBL288445 1 6.20
CHEMBL40816 1 6.19
CHEMBL39417 1 6.00
CHEMBL38742 1 5.98
CHEMBL6393 1 5.98
CHEMBL40879 1 5.90
CHEMBL443258 1 5.78
CHEMBL6385 1 5.29
CHEMBL269073 1 5.23
CHEMBL6503 1 -
CHEMBL41806 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290779 Ki = 58.0 nM 7.24
CHEMBL289061 Ki = 130.0 nM 6.89
CHEMBL38633 Ki = 600.0 nM 6.22
CHEMBL288445 Ki = 630.0 nM 6.20
CHEMBL40816 Ki = 640.0 nM 6.19
CHEMBL39417 Ki = 1000.0 nM 6.00
CHEMBL38742 Ki = 1040.0 nM 5.98
CHEMBL6393 Ki = 1040.0 nM 5.98
CHEMBL40879 Ki = 1250.0 nM 5.90
CHEMBL443258 Ki = 1670.0 nM 5.78
CHEMBL6385 Ki = 5190.0 nM 5.29
CHEMBL269073 Ki = 5830.0 nM 5.23
CHEMBL6503 Ki > 10000.0 nM -
CHEMBL41806 Ki > 10000.0 nM -