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Assay Detail

CHEMBL2175616

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Binding
Inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472) using [3H]-SAM after 30 mins by scintillation counter
ChEMBL ↗
56
Total Activities
56
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

Histone-lysine N-methyltransferase, H3 lysine-79 specific (CHEMBL1795117) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.
Anglin JL, Deng L, Yao Y, Cai G, Liu Z, Jiang H, Cheng G, Chen P, Dong S, Song Y.
J Med Chem (2012) 55 : 8066 -8074
PubMed 22924785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 56 5.97 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171169 — — 1 9.34
CHEMBL2171170 — — 1 9.12
CHEMBL2171171 — — 1 7.92
CHEMBL2171172 — — 1 7.66
CHEMBL2170997 — — 1 7.24
CHEMBL2170993 — — 1 7.16
CHEMBL2171002 — — 1 7.10
CHEMBL2170994 — — 1 7.09
CHEMBL2171000 — — 1 6.89
CHEMBL2170998 — — 1 6.85
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE — 1 6.80
CHEMBL2170995 — — 1 6.72
CHEMBL2170996 — — 1 6.57
CHEMBL2171174 — — 1 6.54
CHEMBL2170992 — — 1 6.46
CHEMBL2170989 — — 1 6.26
CHEMBL2170999 — — 1 6.16
CHEMBL2171001 — — 1 6.00
CHEMBL2170991 — — 1 5.96
CHEMBL2171182 — — 1 5.96
CHEMBL2170985 — — 1 5.72
CHEMBL2171175 — — 1 5.70
CHEMBL2171176 — — 1 5.70
CHEMBL2171168 — — 1 5.57
CHEMBL2171178 — — 1 5.55
CHEMBL2171177 — — 1 5.42
CHEMBL2170988 — — 1 5.35
CHEMBL2170986 — — 1 5.26
CHEMBL2171180 — — 1 5.19
CHEMBL2171179 — — 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171169 — Ki = 0.46 nM 9.34
CHEMBL2171170 — Ki = 0.76 nM 9.12
CHEMBL2171171 — Ki = 12.0 nM 7.92
CHEMBL2171172 — Ki = 22.0 nM 7.66
CHEMBL2170997 — Ki = 58.0 nM 7.24
CHEMBL2170993 — Ki = 70.0 nM 7.16
CHEMBL2171002 — Ki = 80.0 nM 7.10
CHEMBL2170994 — Ki = 82.0 nM 7.09
CHEMBL2171000 — Ki = 130.0 nM 6.89
CHEMBL2170998 — Ki = 140.0 nM 6.85
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE Ki = 160.0 nM 6.80
CHEMBL2170995 — Ki = 190.0 nM 6.72
CHEMBL2170996 — Ki = 270.0 nM 6.57
CHEMBL2171174 — Ki = 290.0 nM 6.54
CHEMBL2170992 — Ki = 350.0 nM 6.46
CHEMBL2170989 — Ki = 550.0 nM 6.26
CHEMBL2170999 — Ki = 690.0 nM 6.16
CHEMBL2171001 — Ki = 1000.0 nM 6.00
CHEMBL2170991 — Ki = 1100.0 nM 5.96
CHEMBL2171182 — Ki = 1100.0 nM 5.96
CHEMBL2170985 — Ki = 1900.0 nM 5.72
CHEMBL2171175 — Ki = 2000.0 nM 5.70
CHEMBL2171176 — Ki = 2000.0 nM 5.70
CHEMBL2171168 — Ki = 2700.0 nM 5.57
CHEMBL2171178 — Ki = 2800.0 nM 5.55
CHEMBL2171177 — Ki = 3800.0 nM 5.42
CHEMBL2170988 — Ki = 4500.0 nM 5.35
CHEMBL2170986 — Ki = 5500.0 nM 5.26
CHEMBL2171180 — Ki = 6500.0 nM 5.19
CHEMBL2171179 — Ki = 7800.0 nM 5.11
CHEMBL2171181 — Ki = 8900.0 nM 5.05
CHEMBL2170984 — Ki = 16000.0 nM 4.80
CHEMBL2170987 — Ki = 17000.0 nM 4.77
CHEMBL2170990 — Ki = 18000.0 nM 4.75
CHEMBL2170979 — Ki = 22000.0 nM 4.66
CHEMBL2170983 — Ki = 22000.0 nM 4.66
CHEMBL563938 — Ki = 25000.0 nM 4.60
CHEMBL2170976 — Ki = 46000.0 nM 4.34
CHEMBL2170977 — Ki = 47000.0 nM 4.33
CHEMBL2170975 — Ki = 50000.0 nM 4.30
CHEMBL538693 — Ki = 100000.0 nM 4.00
CHEMBL2171184 — Ki > 100000.0 nM -
CHEMBL2171183 — Ki > 100000.0 nM -
CHEMBL399890 — Ki > 100000.0 nM -
CHEMBL191917 — Ki > 100000.0 nM -
CHEMBL2171173 — Ki > 100000.0 nM -
CHEMBL193561 — Ki > 100000.0 nM -
CHEMBL2170970 — Ki > 100000.0 nM -
CHEMBL2170971 — Ki > 100000.0 nM -
CHEMBL2170972 — Ki > 100000.0 nM -