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Assay Detail

CHEMBL620729

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

Binding
Binding affinity towards 5-hydroxytryptamine 3 receptor by displacement of [3H]2 in Neuroblastoma-Glioma NG-108-15 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Rosen T, Nagel AA, Rizzi JP, Ives JL, Daffeh JB, Ganong AH, Guarino K, Heym J, McLean S, Nowakowski JT.
J Med Chem (1990) 33 : 2715 -2720
PubMed 2213824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.91 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94117 1 9.54
CHEMBL442382 1 9.51
CHEMBL330293 1 9.06
CHEMBL92643 1 9.02
CHEMBL289060 1 9.00
CHEMBL91158 1 8.82
CHEMBL329322 1 8.70
CHEMBL329154 1 8.70
CHEMBL40260 1 8.48
CHEMBL329793 1 8.43
CHEMBL316108 1 8.31
CHEMBL330485 1 8.15
CHEMBL93963 1 8.06
CHEMBL327431 1 7.57
CHEMBL315664 1 7.54
CHEMBL328321 1 7.47
CHEMBL91429 1 7.21
CHEMBL93729 1 7.02
CHEMBL93179 1 6.96
CHEMBL93339 1 6.57
CHEMBL1947052 1 6.48
CHEMBL329658 1 6.41
CHEMBL314085 1 6.40
CHEMBL316107 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94117 Ki = 0.29 nM 9.54
CHEMBL442382 Ki = 0.31 nM 9.51
CHEMBL330293 Ki = 0.88 nM 9.06
CHEMBL92643 Ki = 0.95 nM 9.02
CHEMBL289060 Ki = 1.0 nM 9.00
CHEMBL91158 Ki = 1.5 nM 8.82
CHEMBL329322 Ki = 2.0 nM 8.70
CHEMBL329154 Ki = 2.0 nM 8.70
CHEMBL40260 Ki = 3.3 nM 8.48
CHEMBL329793 Ki = 3.7 nM 8.43
CHEMBL316108 Ki = 4.9 nM 8.31
CHEMBL330485 Ki = 7.1 nM 8.15
CHEMBL93963 Ki = 8.7 nM 8.06
CHEMBL327431 Ki = 27.0 nM 7.57
CHEMBL315664 Ki = 29.0 nM 7.54
CHEMBL328321 Ki = 34.0 nM 7.47
CHEMBL91429 Ki = 61.0 nM 7.21
CHEMBL93729 Ki = 95.0 nM 7.02
CHEMBL93179 Ki = 110.0 nM 6.96
CHEMBL93339 Ki = 270.0 nM 6.57
CHEMBL1947052 Ki = 329.0 nM 6.48
CHEMBL329658 Ki = 390.0 nM 6.41
CHEMBL314085 Ki = 400.0 nM 6.40
CHEMBL316107 Ki = 430.0 nM 6.37