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Assay Detail

CHEMBL619796

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

Binding
Binding affinity at 5-hydroxytryptamine 3 receptor in rat posterior cortex by [3H]-BRL 43694 displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Derivatives of naphthalimide: new potent conformationally restricted antagonists of 5-HT3 receptors.
Langlois M, Soulier J, Bremont B, Shen S, Rampillon V, Giudice A
Bioorg Med Chem Lett (1992) 2 : 691 -694
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.14 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350824 1 9.82
CHEMBL28992 1 9.70
CHEMBL161069 1 9.30
CHEMBL161922 1 9.05
CHEMBL351218 1 8.66
CHEMBL162123 1 8.64
CHEMBL27846 (R)ZACOPRIDE 1 8.59
CHEMBL348156 1 8.57
CHEMBL159552 1 7.85
CHEMBL159609 1 7.82
CHEMBL159305 1 7.66
CHEMBL350489 1 7.63
CHEMBL160087 1 7.52
CHEMBL346555 1 7.51
CHEMBL350423 1 7.39
CHEMBL349472 1 7.21
CHEMBL351217 1 7.10
CHEMBL161113 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350824 Ki = 0.15 nM 9.82
CHEMBL28992 Ki = 0.2 nM 9.70
CHEMBL161069 Ki = 0.5 nM 9.30
CHEMBL161922 Ki = 0.9 nM 9.05
CHEMBL351218 Ki = 2.2 nM 8.66
CHEMBL162123 Ki = 2.3 nM 8.64
CHEMBL27846 (R)ZACOPRIDE Ki = 2.6 nM 8.59
CHEMBL348156 Ki = 2.7 nM 8.57
CHEMBL159552 Ki = 14.0 nM 7.85
CHEMBL159609 Ki = 15.0 nM 7.82
CHEMBL159305 Ki = 22.0 nM 7.66
CHEMBL350489 Ki = 23.5 nM 7.63
CHEMBL160087 Ki = 30.0 nM 7.52
CHEMBL346555 Ki = 31.0 nM 7.51
CHEMBL350423 Ki = 41.0 nM 7.39
CHEMBL349472 Ki = 61.0 nM 7.21
CHEMBL351217 Ki = 80.0 nM 7.10
CHEMBL161113 Ki = 374.0 nM 6.43