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Assay Detail

CHEMBL617893

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

Binding
Displacement of [H]-mesulergine from CHO cells expressing human 5-hydroxytryptamine 2C receptor.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.
Stevenson GI, Smith AL, Lewis S, Michie SG, Neduvelil JG, Patel S, Marwood R, Patel S, Castro JL.
Bioorg Med Chem Lett (2000) 10 : 2697 -2699
PubMed 11133071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.18 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328595 1 8.08
CHEMBL91549 1 7.96
CHEMBL90911 1 7.92
CHEMBL330303 1 7.82
CHEMBL91446 1 7.54
CHEMBL91197 1 7.52
CHEMBL328459 1 7.51
CHEMBL90263 1 7.44
CHEMBL91463 1 7.44
CHEMBL90837 1 7.44
CHEMBL92416 1 6.92
CHEMBL91542 1 6.80
CHEMBL328257 1 6.80
CHEMBL91447 1 6.75
CHEMBL90739 1 6.64
CHEMBL90347 1 6.58
CHEMBL91205 1 6.57
CHEMBL91122 1 5.52
CHEMBL92417 1 -
CHEMBL90092 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328595 Ki = 8.4 nM 8.08
CHEMBL91549 Ki = 11.0 nM 7.96
CHEMBL90911 Ki = 12.0 nM 7.92
CHEMBL330303 Ki = 15.0 nM 7.82
CHEMBL91446 Ki = 29.0 nM 7.54
CHEMBL91197 Ki = 30.0 nM 7.52
CHEMBL328459 Ki = 31.0 nM 7.51
CHEMBL90263 Ki = 36.0 nM 7.44
CHEMBL91463 Ki = 36.0 nM 7.44
CHEMBL90837 Ki = 36.0 nM 7.44
CHEMBL92416 Ki = 120.0 nM 6.92
CHEMBL91542 Ki = 160.0 nM 6.80
CHEMBL328257 Ki = 160.0 nM 6.80
CHEMBL91447 Ki = 180.0 nM 6.75
CHEMBL90739 Ki = 230.0 nM 6.64
CHEMBL90347 Ki = 260.0 nM 6.58
CHEMBL91205 Ki = 268.0 nM 6.57
CHEMBL91122 Ki = 3000.0 nM 5.52
CHEMBL92417 Ki > 1000.0 nM -
CHEMBL90092 Ki > 1000.0 nM -