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Assay Detail

CHEMBL2157809

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Binding
Binding affinity to 5HT3 receptor
11
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of α7 nicotinic acetylcholine receptor modulators.
Mazurov AA, Speake JD, Yohannes D.
J Med Chem (2011) 54 : 7943 -7961
PubMed 21919481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.72 9.00
IC50 1 6.52 6.52
Kd 1 4.89 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419496 1 9.00
CHEMBL611082 1 7.89
CHEMBL378349 1 6.76
CHEMBL603052 1 6.61
CHEMBL2151572 ENCENICLINE 3.0 1 6.52
CHEMBL379302 1 6.51
CHEMBL597843 1 6.24
CHEMBL378471 1 6.18
CHEMBL597241 1 5.86
CHEMBL563848 1 5.40
CHEMBL499536 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419496 Ki = 1.0 nM 9.00
CHEMBL611082 Ki = 13.0 nM 7.89
CHEMBL378349 Ki = 174.0 nM 6.76
CHEMBL603052 Ki = 244.0 nM 6.61
CHEMBL2151572 ENCENICLINE IC50 = 299.0 nM 6.52
CHEMBL379302 Ki = 310.0 nM 6.51
CHEMBL597843 Ki = 579.0 nM 6.24
CHEMBL378471 Ki = 663.0 nM 6.18
CHEMBL597241 Ki = 1370.0 nM 5.86
CHEMBL563848 Ki = 3993.0 nM 5.40
CHEMBL499536 Kd = 13000.0 nM 4.89