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Assay Detail

CHEMBL5524256

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Binding
Inhibition of N-terminal 3xFlag-tagged recombinant human TET1 catalytic domain (E1418 to V2136 residues) expressed in baculovirus infected Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by substrate and DNA-cofactor addition measured after 30 mins by Alphascreen assay
ChEMBL ↗
38
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methylcytosine dioxygenase TET1 (CHEMBL4523402) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling.
Šimelis K, Saraç H, Salah E, Nishio K, McAllister TE, Corner TP, Tumber A, Belle R, Schofield CJ, Suga H, Kawamura A.
Bioorg Med Chem (2024) 99 : 117597 -117597
PubMed 38262305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.03 7.74
pIC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5527999 — — 2 7.74
CHEMBL5557793 — — 1 6.76
CHEMBL5559263 — — 1 6.71
CHEMBL5549950 — — 1 6.69
CHEMBL5532540 — — 1 6.62
CHEMBL5565375 — — 2 6.60
CHEMBL3785455 — — 1 6.60
CHEMBL5557372 — — 2 6.59
CHEMBL5557587 — — 1 6.57
CHEMBL5561497 — — 1 6.44
CHEMBL5562605 — — 1 6.39
CHEMBL5556063 — — 1 6.38
CHEMBL5567655 — — 1 6.33
CHEMBL1230640 — — 1 6.25
CHEMBL5562105 — — 1 6.22
CHEMBL5561894 — — 1 6.16
CHEMBL5561920 — — 1 6.11
CHEMBL5564944 — — 1 6.10
CHEMBL5549844 — — 1 6.10
CHEMBL5558323 — — 1 5.96
CHEMBL5557957 — — 1 5.94
CHEMBL4203498 — — 1 5.94
CHEMBL5563922 — — 1 5.91
CHEMBL5563232 — — 1 5.87
CHEMBL5561450 — — 1 5.76
CHEMBL5560200 — — 1 5.73
CHEMBL5566835 — — 1 5.54
CHEMBL5564005 — — 1 5.51
CHEMBL5563415 — — 1 5.16
CHEMBL5557758 — — 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5527999 — IC50 = 18.2 nM 7.74
CHEMBL5557793 — IC50 = 173.78 nM 6.76
CHEMBL5559263 — IC50 = 194.98 nM 6.71
CHEMBL5549950 — IC50 = 204.17 nM 6.69
CHEMBL5532540 — IC50 = 239.88 nM 6.62
CHEMBL5527999 — IC50 = 250.0 nM 6.60
CHEMBL5565375 — IC50 = 250.0 nM 6.60
CHEMBL3785455 — IC50 = 251.19 nM 6.60
CHEMBL5557372 — IC50 = 257.04 nM 6.59
CHEMBL5557372 — IC50 = 260.0 nM 6.58
CHEMBL5557587 — IC50 = 269.15 nM 6.57
CHEMBL5561497 — IC50 = 363.08 nM 6.44
CHEMBL5562605 — IC50 = 407.38 nM 6.39
CHEMBL5556063 — IC50 = 416.87 nM 6.38
CHEMBL5567655 — IC50 = 467.74 nM 6.33
CHEMBL1230640 — IC50 = 562.34 nM 6.25
CHEMBL5562105 — IC50 = 602.56 nM 6.22
CHEMBL5561894 — IC50 = 691.83 nM 6.16
CHEMBL5561920 — IC50 = 776.25 nM 6.11
CHEMBL5549844 — IC50 = 794.33 nM 6.10
CHEMBL5564944 — IC50 = 794.33 nM 6.10
CHEMBL5558323 — IC50 = 1096.48 nM 5.96
CHEMBL5557957 — IC50 = 1148.15 nM 5.94
CHEMBL4203498 — IC50 = 1148.15 nM 5.94
CHEMBL5563922 — IC50 = 1230.27 nM 5.91
CHEMBL5563232 — IC50 = 1348.96 nM 5.87
CHEMBL5561450 — IC50 = 1737.8 nM 5.76
CHEMBL5560200 — IC50 = 1862.09 nM 5.73
CHEMBL5566835 — IC50 = 2884.03 nM 5.54
CHEMBL5564005 — IC50 = 3090.3 nM 5.51
CHEMBL5563415 — IC50 = 6918.31 nM 5.16
CHEMBL5557758 — IC50 = 9549.93 nM 5.02
CHEMBL5542479 — IC50 = 10715.19 nM 4.97
CHEMBL5560439 — IC50 = 13803.84 nM 4.86
CHEMBL5564980 — IC50 = 44668.36 nM 4.35
CHEMBL5542589 — IC50 = 70794.58 nM 4.15
CHEMBL5565375 — pIC50 - — -
CHEMBL5565962 — IC50 > 100000.0 nM -