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Assay Detail

CHEMBL617385

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Binding
Affinity against 5-hydroxytryptamine 2A receptor (K) labeled with [3H]ketanserin.
32
Total Activities
32
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 (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.
Glennon RA, Dukat M, el-Bermawy M, Law H, De los Angeles J, Teitler M, King A, Herrick-Davis K.
J Med Chem (1994) 37 : 1929 -1935
PubMed 8027974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.94 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294902 1 8.80
CHEMBL57427 1 8.28
CHEMBL60585 1 7.80
CHEMBL292692 1 7.80
CHEMBL58133 1 7.66
CHEMBL57939 1 7.66
CHEMBL57826 1 7.64
CHEMBL58136 1 7.52
CHEMBL292821 1 7.47
CHEMBL60757 1 7.30
CHEMBL61207 1 7.30
CHEMBL58083 1 7.26
CHEMBL58556 1 7.08
CHEMBL58555 1 7.00
CHEMBL417957 1 7.00
CHEMBL294216 1 6.96
CHEMBL294151 1 6.96
CHEMBL292921 1 6.80
CHEMBL418319 1 6.54
CHEMBL8165 5-METHOXYTRYPTAMINE 1 6.52
CHEMBL57147 1 6.48
CHEMBL57000 1 6.42
CHEMBL294490 1 6.40
CHEMBL58273 1 6.38
CHEMBL58579 1 6.35
CHEMBL58845 1 6.32
CHEMBL433485 1 6.32
CHEMBL293932 1 6.25
CHEMBL7257 MEBUFOTENIN 2.0 1 6.21
CHEMBL299044 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294902 Ki = 1.6 nM 8.80
CHEMBL57427 Ki = 5.2 nM 8.28
CHEMBL60585 Ki = 16.0 nM 7.80
CHEMBL292692 Ki = 16.0 nM 7.80
CHEMBL58133 Ki = 22.0 nM 7.66
CHEMBL57939 Ki = 22.0 nM 7.66
CHEMBL57826 Ki = 23.0 nM 7.64
CHEMBL58136 Ki = 30.0 nM 7.52
CHEMBL292821 Ki = 34.0 nM 7.47
CHEMBL60757 Ki = 50.0 nM 7.30
CHEMBL61207 Ki = 50.0 nM 7.30
CHEMBL58083 Ki = 55.0 nM 7.26
CHEMBL58556 Ki = 84.0 nM 7.08
CHEMBL58555 Ki = 100.0 nM 7.00
CHEMBL417957 Ki = 100.0 nM 7.00
CHEMBL294151 Ki = 110.0 nM 6.96
CHEMBL294216 Ki = 110.0 nM 6.96
CHEMBL292921 Ki = 160.0 nM 6.80
CHEMBL418319 Ki = 290.0 nM 6.54
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 300.0 nM 6.52
CHEMBL57147 Ki = 330.0 nM 6.48
CHEMBL57000 Ki = 380.0 nM 6.42
CHEMBL294490 Ki = 400.0 nM 6.40
CHEMBL58273 Ki = 420.0 nM 6.38
CHEMBL58579 Ki = 450.0 nM 6.35
CHEMBL58845 Ki = 475.0 nM 6.32
CHEMBL433485 Ki = 480.0 nM 6.32
CHEMBL293932 Ki = 565.0 nM 6.25
CHEMBL7257 MEBUFOTENIN Ki = 620.0 nM 6.21
CHEMBL299044 Ki = 895.0 nM 6.05
CHEMBL57888 Ki = 930.0 nM 6.03
CHEMBL293760 Ki = 4260.0 nM 5.37