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Assay Detail

CHEMBL618697

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

Binding
Binding affinity towards cloned rat 5-hydroxytryptamine 2A receptor by [3H]ketanserin displacement.
19
Total Activities
19
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

Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Grella B, Teitler M, Smith C, Herrick-Davis K, Glennon RA.
Bioorg Med Chem Lett (2003) 13 : 4421 -4425
PubMed 14643338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.23 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6857 1 7.66
CHEMBL6746 1 6.96
CHEMBL344051 1 6.91
CHEMBL6586 1 6.89
CHEMBL6426 1 6.75
CHEMBL441891 1 6.62
CHEMBL267599 1 6.41
CHEMBL343079 1 6.33
CHEMBL6591 1 6.33
CHEMBL6427 1 6.30
CHEMBL269571 1 6.19
CHEMBL428999 1 5.88
CHEMBL6626 1 5.76
CHEMBL6717 1 5.62
CHEMBL269367 1 5.49
CHEMBL269236 TRYPTOLINE 1 5.42
CHEMBL6310 1 5.33
CHEMBL266084 1 5.32
CHEMBL6409 CGS-19281A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6857 Ki = 22.0 nM 7.66
CHEMBL6746 Ki = 110.0 nM 6.96
CHEMBL344051 Ki = 124.0 nM 6.91
CHEMBL6586 Ki = 130.0 nM 6.89
CHEMBL6426 Ki = 180.0 nM 6.75
CHEMBL441891 Ki = 240.0 nM 6.62
CHEMBL267599 Ki = 390.0 nM 6.41
CHEMBL343079 Ki = 470.0 nM 6.33
CHEMBL6591 Ki = 470.0 nM 6.33
CHEMBL6427 Ki = 500.0 nM 6.30
CHEMBL269571 Ki = 640.0 nM 6.19
CHEMBL428999 Ki = 1330.0 nM 5.88
CHEMBL6626 Ki = 1720.0 nM 5.76
CHEMBL6717 Ki = 2370.0 nM 5.62
CHEMBL269367 Ki = 3240.0 nM 5.49
CHEMBL269236 TRYPTOLINE Ki = 3800.0 nM 5.42
CHEMBL6310 Ki = 4620.0 nM 5.33
CHEMBL266084 Ki = 4780.0 nM 5.32
CHEMBL6409 CGS-19281A Ki > 10000.0 nM -