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Assay Detail

CHEMBL617481

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

Binding
Binding affinity against 5-hydroxytryptamine 2A receptor
27
Total Activities
27
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

Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding.
Ismaiel AM, Arruda K, Teitler M, Glennon RA.
J Med Chem (1995) 38 : 1196 -1202
PubMed 7707322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.40 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18972 GLEMANSERIN 2.0 1 8.60
CHEMBL417637 1 8.52
CHEMBL19259 1 8.28
CHEMBL18592 1 8.16
CHEMBL19491 1 8.07
CHEMBL19589 1 8.02
CHEMBL19262 1 8.00
CHEMBL416911 1 7.75
CHEMBL273766 1 7.75
CHEMBL18880 1 7.72
CHEMBL19338 1 7.70
CHEMBL18222 1 7.66
CHEMBL18588 1 7.40
CHEMBL19255 1 7.28
CHEMBL19615 1 7.21
CHEMBL18929 1 7.01
CHEMBL415996 1 7.00
CHEMBL276784 1 6.92
CHEMBL18904 1 6.90
CHEMBL18930 1 6.89
CHEMBL18719 1 6.85
CHEMBL19351 1 6.75
CHEMBL19375 1 6.62
CHEMBL18905 1 6.58
CHEMBL18955 1 6.48
CHEMBL19204 1 6.22
CHEMBL278954 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18972 GLEMANSERIN Ki = 2.5 nM 8.60
CHEMBL417637 Ki = 3.0 nM 8.52
CHEMBL19259 Ki = 5.3 nM 8.28
CHEMBL18592 Ki = 6.9 nM 8.16
CHEMBL19491 Ki = 8.5 nM 8.07
CHEMBL19589 Ki = 9.6 nM 8.02
CHEMBL19262 Ki = 10.0 nM 8.00
CHEMBL416911 Ki = 18.0 nM 7.75
CHEMBL273766 Ki = 18.0 nM 7.75
CHEMBL18880 Ki = 19.0 nM 7.72
CHEMBL19338 Ki = 20.0 nM 7.70
CHEMBL18222 Ki = 22.0 nM 7.66
CHEMBL18588 Ki = 40.0 nM 7.40
CHEMBL19255 Ki = 53.0 nM 7.28
CHEMBL19615 Ki = 62.0 nM 7.21
CHEMBL18929 Ki = 98.0 nM 7.01
CHEMBL415996 Ki = 100.0 nM 7.00
CHEMBL276784 Ki = 120.0 nM 6.92
CHEMBL18904 Ki = 126.0 nM 6.90
CHEMBL18930 Ki = 130.0 nM 6.89
CHEMBL18719 Ki = 140.0 nM 6.85
CHEMBL19351 Ki = 180.0 nM 6.75
CHEMBL19375 Ki = 240.0 nM 6.62
CHEMBL18905 Ki = 265.0 nM 6.58
CHEMBL18955 Ki = 330.0 nM 6.48
CHEMBL19204 Ki = 600.0 nM 6.22
CHEMBL278954 Ki < 10000.0 nM -