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Compound Detail

CHEMBL2171170

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CNc1ncnc2c1ncn2[C@@H]1O[C@H](CN(CCCNC(=O)Nc2ccc(C(C)(C)C)cc2)C(C)C)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL2171170
Phase Preclinical
Structure Type MOL
InChI Key ROHQGHWNUHVBHY-HUBRGWSESA-N
4
Targets
7
Activities
3
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

554.7
MW (Da)
2.71
ALogP
10
HBA
5
HBD
149.7
PSA (Ų)
0.24
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H42N8O4
MW 554.70
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.64

Activity Summary

EC50 3 meas. best 5.25
Kd 2 meas. best 7.07
Ki 2 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase, H3 lysine-79 specific
CHEMBL1795117
Ki 9.12 9.11 0.8 2
Histone-lysine N-methyltransferase, H3 lysine-79 specific
CHEMBL1795117
Kd 7.07 6.945 86.0 2
MV4-11
CHEMBL613835
EC50 5.25 5.25 5600.0 1
THP-1
CHEMBL614245
EC50 4.96 4.96 11000.0 1
NB-4
CHEMBL614188
EC50 4.11 4.11 77000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22924785 10.1021/jm300917h MV4-11 5
22924785 10.1021/jm300917h Histone-lysine N-methyltransferase, H3 lysine-79 specific 3
22924785 10.1021/jm300917h Unchecked 3
22924785 10.1021/jm300917h NB-4 1
22924785 10.1021/jm300917h THP-1 1
22924785 10.1021/jm300917h Histone-lysine N-methyltransferase SUV39H1 1
22924785 10.1021/jm300917h Histone-arginine methyltransferase CARM1 1
22924785 10.1021/jm300917h Protein arginine N-methyltransferase 1 1
23879463 10.1021/jm4007752 Histone-lysine N-methyltransferase, H3 lysine-79 specific 1

Data from ChEMBL 36 via Core Engine