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Assay Detail

CHEMBL4195563

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Binding
Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay
ChEMBL ↗
50
Total Activities
47
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

DNA (cytosine-5)-methyltransferase 1 (CHEMBL1993) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.
Rabal O, Sánchez-Arias JA, San José-Enériz E, Agirre X, de Miguel I, Garate L, Miranda E, Sáez E, Roa S, Martínez-Climent JA, Liu Y, Wu W, Xu M, Prosper F, Oyarzabal J.
J Med Chem (2018) 61 : 6546 -6573
PubMed 29890830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.49 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215326 — — 1 7.68
CHEMBL4208004 — — 1 7.50
CHEMBL4212905 — — 1 7.40
CHEMBL4208010 — — 1 7.14
CHEMBL4211688 — — 1 7.10
CHEMBL4203133 — — 1 7.08
CHEMBL4215862 — — 1 7.08
CHEMBL4208812 — — 2 6.91
CHEMBL4206035 — — 1 6.85
CHEMBL4216593 — — 1 6.73
CHEMBL4213346 — — 1 6.70
CHEMBL4216144 — — 1 6.70
CHEMBL4203647 — — 1 6.69
CHEMBL4204482 — — 1 6.68
CHEMBL4205136 — — 1 6.67
CHEMBL4203933 — — 2 6.66
CHEMBL4207331 — — 1 6.63
CHEMBL4205373 — — 1 6.63
CHEMBL4160008 — — 1 6.63
CHEMBL4210033 — — 1 6.61
CHEMBL4204903 — — 1 6.60
CHEMBL4216663 — — 1 6.58
CHEMBL4212218 — — 2 6.54
CHEMBL4215377 — — 1 6.53
CHEMBL4217332 — — 1 6.53
CHEMBL4170114 — — 1 6.42
CHEMBL4203655 — — 1 6.38
CHEMBL4207526 — — 1 6.37
CHEMBL4212380 — — 1 6.35
CHEMBL4208425 — — 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215326 — IC50 = 21.0 nM 7.68
CHEMBL4208004 — IC50 = 32.0 nM 7.50
CHEMBL4212905 — IC50 = 40.0 nM 7.40
CHEMBL4208010 — IC50 = 73.0 nM 7.14
CHEMBL4211688 — IC50 = 80.0 nM 7.10
CHEMBL4203133 — IC50 = 83.0 nM 7.08
CHEMBL4215862 — IC50 = 83.0 nM 7.08
CHEMBL4208812 — IC50 = 123.0 nM 6.91
CHEMBL4206035 — IC50 = 140.0 nM 6.85
CHEMBL4216593 — IC50 = 187.0 nM 6.73
CHEMBL4216144 — IC50 = 201.0 nM 6.70
CHEMBL4213346 — IC50 = 200.0 nM 6.70
CHEMBL4203647 — IC50 = 205.0 nM 6.69
CHEMBL4204482 — IC50 = 211.0 nM 6.68
CHEMBL4205136 — IC50 = 212.0 nM 6.67
CHEMBL4203933 — IC50 = 220.0 nM 6.66
CHEMBL4207331 — IC50 = 235.0 nM 6.63
CHEMBL4205373 — IC50 = 234.0 nM 6.63
CHEMBL4160008 — IC50 = 234.0 nM 6.63
CHEMBL4210033 — IC50 = 247.0 nM 6.61
CHEMBL4204903 — IC50 = 250.0 nM 6.60
CHEMBL4216663 — IC50 = 261.0 nM 6.58
CHEMBL4212218 — IC50 = 290.0 nM 6.54
CHEMBL4217332 — IC50 = 297.0 nM 6.53
CHEMBL4215377 — IC50 = 298.0 nM 6.53
CHEMBL4208812 — IC50 = 316.23 nM 6.50
CHEMBL4212218 — IC50 = 316.23 nM 6.50
CHEMBL4203933 — IC50 = 316.23 nM 6.50
CHEMBL4170114 — IC50 = 382.0 nM 6.42
CHEMBL4203655 — IC50 = 414.0 nM 6.38
CHEMBL4207526 — IC50 = 425.0 nM 6.37
CHEMBL4212380 — IC50 = 446.0 nM 6.35
CHEMBL4208425 — IC50 = 475.0 nM 6.32
CHEMBL4210910 — IC50 = 494.0 nM 6.31
CHEMBL4209267 — IC50 = 501.0 nM 6.30
CHEMBL4203186 — IC50 = 588.0 nM 6.23
CHEMBL4217747 — IC50 = 624.0 nM 6.21
CHEMBL4210432 — IC50 = 645.0 nM 6.19
CHEMBL4208522 — IC50 = 722.0 nM 6.14
CHEMBL4202651 — IC50 = 750.0 nM 6.12
CHEMBL4205107 — IC50 = 781.0 nM 6.11
CHEMBL4207483 — IC50 = 833.0 nM 6.08
CHEMBL4210955 — IC50 = 950.0 nM 6.02
CHEMBL4211622 — IC50 = 1030.0 nM 5.99
CHEMBL4212375 — IC50 = 1080.0 nM 5.97
CHEMBL4217087 — IC50 = 1320.0 nM 5.88
CHEMBL4216799 — IC50 = 1790.0 nM 5.75
CHEMBL4206071 — IC50 = 1870.0 nM 5.73
CHEMBL1231795 — IC50 = 2010.0 nM 5.70
CHEMBL4214834 — IC50 = 2080.0 nM 5.68