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Assay Detail

CHEMBL747899

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

Functional
Effective concentration against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Cell Type NG108-15
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
Campiani G, Morelli E, Gemma S, Nacci V, Butini S, Hamon M, Novellino E, Greco G, Cagnotto A, Goegan M, Cervo L, Dalla Valle F, Fracasso C, Caccia S, Mennini T.
J Med Chem (1999) 42 : 4362 -4379
PubMed 10543880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18772 QUIPAZINE 2.0 1 9.00
CHEMBL139327 1 8.80
CHEMBL423899 1 8.77
CHEMBL136449 1 8.62
CHEMBL136090 1 8.57
CHEMBL341474 1 8.52
CHEMBL136978 1 8.42
CHEMBL137621 1 8.38
CHEMBL342447 1 8.38
CHEMBL337324 1 8.18
CHEMBL136524 1 8.14
CHEMBL342690 1 8.02
CHEMBL136536 1 7.92
CHEMBL422279 1 7.85
CHEMBL136525 1 7.82
CHEMBL53573 1 7.50
CHEMBL136108 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18772 QUIPAZINE EC50 = 1.0 nM 9.00
CHEMBL139327 EC50 = 1.6 nM 8.80
CHEMBL423899 EC50 = 1.7 nM 8.77
CHEMBL136449 EC50 = 2.4 nM 8.62
CHEMBL136090 EC50 = 2.7 nM 8.57
CHEMBL341474 EC50 = 3.0 nM 8.52
CHEMBL136978 EC50 = 3.8 nM 8.42
CHEMBL137621 EC50 = 4.2 nM 8.38
CHEMBL342447 EC50 = 4.2 nM 8.38
CHEMBL337324 EC50 = 6.6 nM 8.18
CHEMBL136524 EC50 = 7.2 nM 8.14
CHEMBL342690 EC50 = 9.5 nM 8.02
CHEMBL136536 EC50 = 12.0 nM 7.92
CHEMBL422279 EC50 = 14.0 nM 7.85
CHEMBL136525 EC50 = 15.0 nM 7.82
CHEMBL53573 EC50 = 32.0 nM 7.50
CHEMBL136108 EC50 = 54.0 nM 7.27