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Assay Detail

CHEMBL617709

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

Binding
Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor from rat cortical homogenate using [3H]zacopride as radioligand
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

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
IC50 43 7.65 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139327 1 9.17
CHEMBL136978 1 9.10
CHEMBL341474 1 9.09
CHEMBL54914 1 9.00
CHEMBL342690 1 8.95
CHEMBL136090 1 8.80
CHEMBL137621 1 8.66
CHEMBL53573 1 8.64
CHEMBL136449 1 8.59
CHEMBL137565 1 8.51
CHEMBL337101 1 8.44
CHEMBL18772 QUIPAZINE 2.0 1 8.42
CHEMBL136525 1 8.42
CHEMBL136524 1 8.28
CHEMBL335803 1 8.18
CHEMBL46 ONDANSETRON 4.0 1 8.17
CHEMBL136108 1 8.09
CHEMBL136536 1 8.06
CHEMBL337324 1 7.96
CHEMBL137564 1 7.92
CHEMBL342447 1 7.89
CHEMBL136979 1 7.79
CHEMBL422279 1 7.75
CHEMBL138849 1 7.66
CHEMBL343919 1 7.62
CHEMBL134473 1 7.52
CHEMBL140295 1 7.42
CHEMBL136416 1 7.36
CHEMBL423719 1 7.22
CHEMBL2107804 BEMESETRON 2.0 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139327 IC50 = 0.67 nM 9.17
CHEMBL136978 IC50 = 0.79 nM 9.10
CHEMBL341474 IC50 = 0.81 nM 9.09
CHEMBL54914 IC50 = 1.0 nM 9.00
CHEMBL342690 IC50 = 1.13 nM 8.95
CHEMBL136090 IC50 = 1.6 nM 8.80
CHEMBL137621 IC50 = 2.2 nM 8.66
CHEMBL53573 IC50 = 2.3 nM 8.64
CHEMBL136449 IC50 = 2.6 nM 8.59
CHEMBL137565 IC50 = 3.1 nM 8.51
CHEMBL337101 IC50 = 3.6 nM 8.44
CHEMBL136525 IC50 = 3.8 nM 8.42
CHEMBL18772 QUIPAZINE IC50 = 3.8 nM 8.42
CHEMBL136524 IC50 = 5.2 nM 8.28
CHEMBL335803 IC50 = 6.6 nM 8.18
CHEMBL46 ONDANSETRON IC50 = 6.8 nM 8.17
CHEMBL136108 IC50 = 8.2 nM 8.09
CHEMBL136536 IC50 = 8.8 nM 8.06
CHEMBL337324 IC50 = 11.0 nM 7.96
CHEMBL137564 IC50 = 12.0 nM 7.92
CHEMBL342447 IC50 = 13.0 nM 7.89
CHEMBL136979 IC50 = 16.4 nM 7.79
CHEMBL422279 IC50 = 18.0 nM 7.75
CHEMBL138849 IC50 = 22.0 nM 7.66
CHEMBL343919 IC50 = 24.0 nM 7.62
CHEMBL134473 IC50 = 30.0 nM 7.52
CHEMBL140295 IC50 = 38.0 nM 7.42
CHEMBL136416 IC50 = 44.0 nM 7.36
CHEMBL423719 IC50 = 60.0 nM 7.22
CHEMBL2107804 BEMESETRON IC50 = 97.0 nM 7.01
CHEMBL136772 IC50 = 97.0 nM 7.01
CHEMBL136138 IC50 = 104.0 nM 6.98
CHEMBL342381 IC50 = 104.0 nM 6.98
CHEMBL139534 IC50 = 113.0 nM 6.95
CHEMBL139271 IC50 = 118.0 nM 6.93
CHEMBL424662 IC50 = 148.0 nM 6.83
CHEMBL136266 IC50 = 225.0 nM 6.65
CHEMBL138034 IC50 = 690.0 nM 6.16
CHEMBL334462 IC50 = 780.0 nM 6.11
CHEMBL136666 IC50 = 920.0 nM 6.04
CHEMBL134970 IC50 = 1930.0 nM 5.71
CHEMBL424471 IC50 = 3650.0 nM 5.44
CHEMBL336699 IC50 = 3800.0 nM 5.42