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Assay Detail

CHEMBL1670618

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Functional
Antagonist activity at 5-HT3 receptor in guinea pig ileum muscle
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL3666)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery of new anti-depressants from structurally novel 5-HT3 receptor antagonists: design, synthesis and pharmacological evaluation of 3-ethoxyquinoxalin-2-carboxamides.
Mahesh R, Devadoss T, Pandey DK, Bhatt S.
Bioorg Med Chem Lett (2011) 21 : 1253 -1256
PubMed 21256009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 16 6.16 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668031 1 7.70
CHEMBL1668032 1 7.50
CHEMBL1668036 1 7.20
CHEMBL1668024 1 7.00
CHEMBL46 ONDANSETRON 4.0 1 6.90
CHEMBL1668034 1 6.90
CHEMBL1668033 1 6.80
CHEMBL1668025 1 6.80
CHEMBL1668027 1 6.60
CHEMBL1668026 1 6.00
CHEMBL1668028 1 5.10
CHEMBL1668037 1 5.00
CHEMBL1668023 1 5.00
CHEMBL1668029 1 4.80
CHEMBL1668035 1 4.70
CHEMBL1668030 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668031 Kd = 19.95 nM 7.70
CHEMBL1668032 Kd = 31.62 nM 7.50
CHEMBL1668036 Kd = 63.1 nM 7.20
CHEMBL1668024 Kd = 100.0 nM 7.00
CHEMBL46 ONDANSETRON Kd = 125.89 nM 6.90
CHEMBL1668034 Kd = 125.89 nM 6.90
CHEMBL1668033 Kd = 158.49 nM 6.80
CHEMBL1668025 Kd = 158.49 nM 6.80
CHEMBL1668027 Kd = 251.19 nM 6.60
CHEMBL1668026 Kd = 1000.0 nM 6.00
CHEMBL1668028 Kd = 7943.28 nM 5.10
CHEMBL1668037 Kd = 10000.0 nM 5.00
CHEMBL1668023 Kd = 10000.0 nM 5.00
CHEMBL1668029 Kd = 15848.93 nM 4.80
CHEMBL1668035 Kd = 19952.62 nM 4.70
CHEMBL1668030 Kd = 25118.86 nM 4.60