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Assay Detail

CHEMBL3412050

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

Binding
Inhibition of Notch1 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neurogenic locus notch homolog protein 1 (CHEMBL2146346)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.
Shan W, Balog A, Quesnelle C, Gill P, Han WC, Norris D, Mandal S, Thiruvenkadam R, Gona KB, Thiyagarajan K, Kandula S, McGlinchey K, Menard K, Wen ML, Rose A, White R, Guarino V, Shen DR, Cvijic ME, Ranasinghe A, Dai J, Zhang Y, Wu DR, Mathur A, Rampulla R, Trainor G, Hunt JT, Vite GD, Westhouse R, Lee FY, Gavai AV.
Bioorg Med Chem Lett (2015) 25 : 1905 -1909
PubMed 25857941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3410153 1 9.00
CHEMBL3410163 1 9.00
CHEMBL3410169 1 9.00
CHEMBL3410151 1 8.70
CHEMBL3410170 1 8.70
CHEMBL3410167 1 8.70
CHEMBL3410168 1 8.70
CHEMBL3410152 1 8.52
CHEMBL3410160 1 8.52
CHEMBL3410162 1 8.52
CHEMBL3410164 1 8.52
CHEMBL3410161 1 8.40
CHEMBL3410166 1 8.05
CHEMBL3410154 1 7.89
CHEMBL3410157 1 7.50
CHEMBL3410159 1 7.27
CHEMBL3410158 1 6.77
CHEMBL3410156 1 6.64
CHEMBL3410155 1 5.92
CHEMBL3410165 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3410153 IC50 = 1.0 nM 9.00
CHEMBL3410163 IC50 = 1.0 nM 9.00
CHEMBL3410169 IC50 = 1.0 nM 9.00
CHEMBL3410151 IC50 = 2.0 nM 8.70
CHEMBL3410170 IC50 = 2.0 nM 8.70
CHEMBL3410167 IC50 = 2.0 nM 8.70
CHEMBL3410168 IC50 = 2.0 nM 8.70
CHEMBL3410152 IC50 = 3.0 nM 8.52
CHEMBL3410160 IC50 = 3.0 nM 8.52
CHEMBL3410162 IC50 = 3.0 nM 8.52
CHEMBL3410164 IC50 = 3.0 nM 8.52
CHEMBL3410161 IC50 = 4.0 nM 8.40
CHEMBL3410166 IC50 = 9.0 nM 8.05
CHEMBL3410154 IC50 = 13.0 nM 7.89
CHEMBL3410157 IC50 = 32.0 nM 7.50
CHEMBL3410159 IC50 = 54.0 nM 7.27
CHEMBL3410158 IC50 = 169.0 nM 6.77
CHEMBL3410156 IC50 = 231.0 nM 6.64
CHEMBL3410155 IC50 = 1190.0 nM 5.92
CHEMBL3410165 IC50 = 2060.0 nM 5.69