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Assay Detail

CHEMBL618895

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

Binding
Binding affinity towards rat 5-hydroxytryptamine 2A receptor expressed in NIH3T3 cells using [3H]ketanserin as radioligand
32
Total Activities
32
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

Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.
Khorana N, Smith C, Herrick-Davis K, Purohit A, Teitler M, Grella B, Dukat M, Glennon RA.
J Med Chem (2003) 46 : 3930 -3937
PubMed 12930153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.98 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129230 1 8.22
CHEMBL129163 1 7.80
CHEMBL126438 1 7.70
CHEMBL129476 1 7.66
CHEMBL96504 1 7.52
CHEMBL128185 1 7.42
CHEMBL126138 1 7.42
CHEMBL424258 1 7.30
CHEMBL128099 1 7.30
CHEMBL446356 1 7.22
CHEMBL130586 1 7.19
CHEMBL341506 1 7.19
CHEMBL128848 1 7.16
CHEMBL340646 1 7.00
CHEMBL126898 1 6.94
CHEMBL2111848 1 6.92
CHEMBL128184 1 6.92
CHEMBL338095 1 6.89
CHEMBL125417 1 6.89
CHEMBL126823 1 6.82
CHEMBL338696 1 6.80
CHEMBL126994 1 6.76
CHEMBL125361 1 6.73
CHEMBL126897 1 6.71
CHEMBL126737 1 6.68
CHEMBL338081 1 6.65
CHEMBL130585 1 6.55
CHEMBL435814 1 6.54
CHEMBL128945 1 6.38
CHEMBL340511 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129230 Ki = 6.0 nM 8.22
CHEMBL129163 Ki = 16.0 nM 7.80
CHEMBL126438 Ki = 20.0 nM 7.70
CHEMBL129476 Ki = 22.0 nM 7.66
CHEMBL96504 Ki = 30.0 nM 7.52
CHEMBL128185 Ki = 38.0 nM 7.42
CHEMBL126138 Ki = 38.0 nM 7.42
CHEMBL424258 Ki = 50.0 nM 7.30
CHEMBL128099 Ki = 50.0 nM 7.30
CHEMBL446356 Ki = 60.0 nM 7.22
CHEMBL130586 Ki = 65.0 nM 7.19
CHEMBL341506 Ki = 65.0 nM 7.19
CHEMBL128848 Ki = 70.0 nM 7.16
CHEMBL340646 Ki = 100.0 nM 7.00
CHEMBL126898 Ki = 115.0 nM 6.94
CHEMBL128184 Ki = 120.0 nM 6.92
CHEMBL2111848 Ki = 120.0 nM 6.92
CHEMBL338095 Ki = 130.0 nM 6.89
CHEMBL125417 Ki = 130.0 nM 6.89
CHEMBL126823 Ki = 150.0 nM 6.82
CHEMBL338696 Ki = 160.0 nM 6.80
CHEMBL126994 Ki = 175.0 nM 6.76
CHEMBL125361 Ki = 185.0 nM 6.73
CHEMBL126897 Ki = 195.0 nM 6.71
CHEMBL126737 Ki = 210.0 nM 6.68
CHEMBL338081 Ki = 225.0 nM 6.65
CHEMBL130585 Ki = 280.0 nM 6.55
CHEMBL435814 Ki = 285.0 nM 6.54
CHEMBL128945 Ki = 415.0 nM 6.38
CHEMBL340511 Ki = 480.0 nM 6.32
CHEMBL126188 Ki = 625.0 nM 6.20
CHEMBL92879 Ki = 3100.0 nM 5.51