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Compound Detail

CHEMBL4065181

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COc1ccc(-c2nn3c(-c4cccs4)nnc3s2)cc1OC

Basic Information

ChEMBL ID CHEMBL4065181
Phase Preclinical
Structure Type MOL
InChI Key YTGYWPTWNBGCLG-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
14
Publications
0
Known Names

Molecular Properties

344.4
MW (Da)
3.60
ALogP
8
HBA
0
HBD
61.5
PSA (Ų)
0.57
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12N4O2S2
MW 344.42
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -2.27

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
dCTP pyrophosphatase 1
CHEMBL3769292
IC50 7.7 7.7 20.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.01667 hr Mus musculus
T1/2 0.06667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28145708 10.1021/acs.jmedchem.6b01786 Unchecked 9
28145708 10.1021/acs.jmedchem.6b01786 dCTP pyrophosphatase 1 4
28145708 10.1021/acs.jmedchem.6b01786 No relevant target 4
28145708 10.1021/acs.jmedchem.6b01786 Liver 4
28145708 10.1021/acs.jmedchem.6b01786 ADMET 1
28145708 10.1021/acs.jmedchem.6b01786 Oxidized purine nucleoside triphosphate hydrolase 1
28145708 10.1021/acs.jmedchem.6b01786 Bis(5'-nucleosyl)-tetraphosphatase [asymmetrical] 1
28145708 10.1021/acs.jmedchem.6b01786 ADP-sugar pyrophosphatase 1
28145708 10.1021/acs.jmedchem.6b01786 Uridine diphosphate glucose pyrophosphatase NUDT14 1
28145708 10.1021/acs.jmedchem.6b01786 ADP-ribose pyrophosphatase, mitochondrial 1
28145708 10.1021/acs.jmedchem.6b01786 Nucleotide triphosphate diphosphatase NUDT15 1
28145708 10.1021/acs.jmedchem.6b01786 Inosine triphosphate pyrophosphatase 1
28145708 10.1021/acs.jmedchem.6b01786 HL-60 1
28687206 10.1016/j.bmcl.2017.06.038 dCTP pyrophosphatase 1 1

Data from ChEMBL 36 via Core Engine