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Assay Detail

CHEMBL5534754

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

Binding
Inhibition of human recombinant MYT1 incubated for 60 mins in presence of tracer178 by HTRF analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Myelin transcription factor 1 (CHEMBL2331044)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Tetrahydropyrazolopyrazine Derivatives as Potent and Selective MYT1 Inhibitors for the Treatment of Cancer.
Wang Y, Wang C, Liu T, Qi H, Chen S, Cai X, Zhang M, Aliper A, Ren F, Ding X, Zhavoronkov A.
J Med Chem (2024) 67 : 420 -432
PubMed 38146659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.80 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199076 LUNRESERTIB 2.0 1 8.82
CHEMBL5562687 1 8.72
CHEMBL5566629 1 8.59
CHEMBL5200005 1 8.54
CHEMBL5573176 1 8.44
CHEMBL5572884 1 8.38
CHEMBL5569464 1 8.37
CHEMBL5573390 1 8.34
CHEMBL5575890 1 8.32
CHEMBL5567277 1 8.32
CHEMBL5573971 1 8.31
CHEMBL5569840 1 8.26
CHEMBL5571889 1 8.24
CHEMBL5573662 1 8.18
CHEMBL5563675 1 8.15
CHEMBL5570485 1 7.99
CHEMBL5566455 1 7.98
CHEMBL5565137 1 7.94
CHEMBL5564808 1 7.79
CHEMBL5566287 1 7.76
CHEMBL5574963 1 7.63
CHEMBL5571632 1 7.60
CHEMBL5572439 1 7.31
CHEMBL5573978 1 7.16
CHEMBL5574840 1 6.65
CHEMBL5569793 1 6.45
CHEMBL5570533 1 6.15
CHEMBL5572096 1 5.92
CHEMBL5593294 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199076 LUNRESERTIB IC50 = 1.5 nM 8.82
CHEMBL5562687 IC50 = 1.9 nM 8.72
CHEMBL5566629 IC50 = 2.6 nM 8.59
CHEMBL5200005 IC50 = 2.9 nM 8.54
CHEMBL5573176 IC50 = 3.6 nM 8.44
CHEMBL5572884 IC50 = 4.2 nM 8.38
CHEMBL5569464 IC50 = 4.3 nM 8.37
CHEMBL5573390 IC50 = 4.6 nM 8.34
CHEMBL5575890 IC50 = 4.8 nM 8.32
CHEMBL5567277 IC50 = 4.8 nM 8.32
CHEMBL5573971 IC50 = 4.9 nM 8.31
CHEMBL5569840 IC50 = 5.5 nM 8.26
CHEMBL5571889 IC50 = 5.8 nM 8.24
CHEMBL5573662 IC50 = 6.6 nM 8.18
CHEMBL5563675 IC50 = 7.1 nM 8.15
CHEMBL5570485 IC50 = 10.3 nM 7.99
CHEMBL5566455 IC50 = 10.4 nM 7.98
CHEMBL5565137 IC50 = 11.4 nM 7.94
CHEMBL5564808 IC50 = 16.2 nM 7.79
CHEMBL5566287 IC50 = 17.3 nM 7.76
CHEMBL5574963 IC50 = 23.2 nM 7.63
CHEMBL5571632 IC50 = 25.3 nM 7.60
CHEMBL5572439 IC50 = 48.9 nM 7.31
CHEMBL5573978 IC50 = 69.0 nM 7.16
CHEMBL5574840 IC50 = 222.9 nM 6.65
CHEMBL5569793 IC50 = 359.1 nM 6.45
CHEMBL5570533 IC50 = 713.8 nM 6.15
CHEMBL5572096 IC50 = 1213.0 nM 5.92
CHEMBL5593294 IC50 = 1495.0 nM 5.83