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Assay Detail

CHEMBL620723

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

Binding
Concentration that inhibits the binding of radioligand, [3H]-ICS 205930, to 5-hydroxytryptamine 3 receptor from rat cortex
41
Total Activities
41
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

Synthesis of a new class of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists.
Turconi M, Nicola M, Quintero MG, Maiocchi L, Micheletti R, Giraldo E, Donetti A.
J Med Chem (1990) 33 : 2101 -2108
PubMed 1695682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 7.90 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63742 1 9.05
CHEMBL540017 1 8.81
CHEMBL293239 1 8.77
CHEMBL56564 TROPISETRON 3.0 1 8.77
CHEMBL64986 1 8.68
CHEMBL539262 1 8.66
CHEMBL544755 1 8.64
CHEMBL293468 1 8.43
CHEMBL542869 1 8.10
CHEMBL543340 1 7.92
CHEMBL554389 1 7.79
CHEMBL545449 1 7.75
CHEMBL63891 1 7.70
CHEMBL306003 1 7.67
CHEMBL2107804 BEMESETRON 2.0 1 7.61
CHEMBL541040 1 7.58
CHEMBL63409 1 7.47
CHEMBL539003 1 7.47
CHEMBL552824 1 7.14
CHEMBL65226 1 6.89
CHEMBL555995 1 6.51
CHEMBL418673 1 6.36
CHEMBL63621 1 -
CHEMBL67403 1 -
CHEMBL542634 1 -
CHEMBL552854 1 -
CHEMBL539006 1 -
CHEMBL555088 1 -
CHEMBL539261 1 -
CHEMBL538247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63742 Ki = 0.89 nM 9.05
CHEMBL540017 Ki = 1.53 nM 8.81
CHEMBL56564 TROPISETRON Ki = 1.71 nM 8.77
CHEMBL293239 Ki = 1.7 nM 8.77
CHEMBL64986 Ki = 2.07 nM 8.68
CHEMBL539262 Ki = 2.17 nM 8.66
CHEMBL544755 Ki = 2.3 nM 8.64
CHEMBL293468 Ki = 3.75 nM 8.43
CHEMBL542869 Ki = 7.94 nM 8.10
CHEMBL543340 Ki = 12.0 nM 7.92
CHEMBL554389 Ki = 16.3 nM 7.79
CHEMBL545449 Ki = 18.0 nM 7.75
CHEMBL63891 Ki = 20.2 nM 7.70
CHEMBL306003 Ki = 21.4 nM 7.67
CHEMBL2107804 BEMESETRON Ki = 24.4 nM 7.61
CHEMBL541040 Ki = 26.2 nM 7.58
CHEMBL63409 Ki = 33.6 nM 7.47
CHEMBL539003 Ki = 33.9 nM 7.47
CHEMBL552824 Ki = 72.4 nM 7.14
CHEMBL65226 Ki = 130.0 nM 6.89
CHEMBL555995 Ki = 306.0 nM 6.51
CHEMBL418673 Ki = 436.0 nM 6.36
CHEMBL554844 Ki > 1000.0 nM -
CHEMBL539005 Ki > 1000.0 nM -
CHEMBL540782 Ki > 1000.0 nM -
CHEMBL541283 Ki > 1000.0 nM -
CHEMBL68348 Ki > 1000.0 nM -
CHEMBL555791 Ki > 1000.0 nM -
CHEMBL553266 Ki > 1000.0 nM -
CHEMBL66972 Ki > 1000.0 nM -
CHEMBL554755 Ki > 1000.0 nM -
CHEMBL303463 Ki > 1000.0 nM -
CHEMBL304382 Ki > 1000.0 nM -
CHEMBL538247 Ki > 1000.0 nM -
CHEMBL539261 Ki > 1000.0 nM -
CHEMBL555088 Ki > 1000.0 nM -
CHEMBL539006 Ki > 1000.0 nM -
CHEMBL552854 Ki > 1000.0 nM -
CHEMBL542634 Ki > 1000.0 nM -
CHEMBL67403 Ki > 1000.0 nM -
CHEMBL63621 Ki > 1000.0 nM -