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Assay Detail

CHEMBL976148

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

Binding
Displacement of [3H]dofetilide human ERG expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
Bromidge SM, Bertani B, Borriello M, Bozzoli A, Faedo S, Gianotti M, Gordon LJ, Hill M, Zucchelli V, Watson JM, Zonzini L.
Bioorg Med Chem Lett (2009) 19 : 2338 -2342
PubMed 19286377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.67 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490417 1 7.20
CHEMBL512724 1 7.00
CHEMBL511279 1 6.40
CHEMBL470849 1 6.20
CHEMBL522257 1 6.10
CHEMBL469568 1 5.80
CHEMBL469995 1 5.80
CHEMBL513715 1 5.60
CHEMBL470217 1 5.50
CHEMBL513875 1 5.50
CHEMBL472289 1 5.50
CHEMBL469345 1 5.40
CHEMBL469374 1 5.40
CHEMBL469567 1 5.30
CHEMBL469375 1 5.30
CHEMBL469376 1 5.20
CHEMBL469589 1 5.20
CHEMBL472290 1 5.10
CHEMBL511815 1 5.00
CHEMBL471047 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490417 Ki = 63.1 nM 7.20
CHEMBL512724 Ki = 100.0 nM 7.00
CHEMBL511279 Ki = 398.11 nM 6.40
CHEMBL470849 Ki = 630.96 nM 6.20
CHEMBL522257 Ki = 794.33 nM 6.10
CHEMBL469568 Ki = 1584.89 nM 5.80
CHEMBL469995 Ki = 1584.89 nM 5.80
CHEMBL513715 Ki = 2511.89 nM 5.60
CHEMBL470217 Ki = 3162.28 nM 5.50
CHEMBL513875 Ki = 3162.28 nM 5.50
CHEMBL472289 Ki = 3162.28 nM 5.50
CHEMBL469345 Ki = 3981.07 nM 5.40
CHEMBL469374 Ki = 3981.07 nM 5.40
CHEMBL469567 Ki = 5011.87 nM 5.30
CHEMBL469375 Ki = 5011.87 nM 5.30
CHEMBL469376 Ki = 6309.57 nM 5.20
CHEMBL469589 Ki = 6309.57 nM 5.20
CHEMBL472290 Ki = 7943.28 nM 5.10
CHEMBL511815 Ki = 10000.0 nM 5.00
CHEMBL471047 Ki = 12589.25 nM 4.90