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Assay Detail

CHEMBL861445

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Binding
Binding affinity to human 5HT2C
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A new class of selective, non-basic 5-HT2A receptor antagonists.
Ladduwahetty T, Boase AL, Mitchinson A, Quin C, Patel S, Chapman K, MacLeod AM.
Bioorg Med Chem Lett (2006) 16 : 3201 -3204
PubMed 16632354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.52 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207386 1 7.55
CHEMBL206307 1 7.16
CHEMBL358075 1 7.04
CHEMBL206308 1 7.02
CHEMBL210230 1 6.96
CHEMBL380682 1 6.74
CHEMBL209415 1 6.62
CHEMBL210413 1 6.39
CHEMBL210849 1 6.35
CHEMBL207566 1 6.25
CHEMBL207064 1 6.09
CHEMBL383530 1 6.00
CHEMBL379850 1 5.69
CHEMBL207850 1 5.42
CHEMBL382146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207386 Ki = 28.0 nM 7.55
CHEMBL206307 Ki = 70.0 nM 7.16
CHEMBL358075 Ki = 92.0 nM 7.04
CHEMBL206308 Ki = 96.0 nM 7.02
CHEMBL210230 Ki = 110.0 nM 6.96
CHEMBL380682 Ki = 184.0 nM 6.74
CHEMBL209415 Ki = 239.0 nM 6.62
CHEMBL210413 Ki = 404.0 nM 6.39
CHEMBL210849 Ki = 449.0 nM 6.35
CHEMBL207566 Ki = 557.0 nM 6.25
CHEMBL207064 Ki = 806.0 nM 6.09
CHEMBL383530 Ki = 997.0 nM 6.00
CHEMBL379850 Ki = 2033.0 nM 5.69
CHEMBL207850 Ki = 3785.0 nM 5.42
CHEMBL382146 Ki > 4000.0 nM -