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Compound Detail

CHEMBL274713

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CCCSc1nc(N[C@@H]2C[C@H]2c2ccccc2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1

Basic Information

ChEMBL ID CHEMBL274713
Phase Preclinical
Structure Type MOL
InChI Key WAAZWZXNFNZGJV-NGIYPOHESA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

486.6
MW (Da)
1.74
ALogP
11
HBA
4
HBD
138.4
PSA (Ų)
0.25
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 C23H30N6O4S
MW 486.60
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.51

Activity Summary

Ki 1 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 12
CHEMBL2001
Ki 8.5 8.5 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 mL.min-1.g-1 Homo sapiens
F 26.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17827008 10.1016/j.bmcl.2007.07.057 Hepatocyte 2
- 10.6019/CHEMBL3301361 No relevant target 2
17827008 10.1016/j.bmcl.2007.07.057 P2Y purinoceptor 12 1
17827008 10.1016/j.bmcl.2007.07.057 Rattus norvegicus 1
- 10.6019/CHEMBL3301361 ADMET 1
32916314 10.1016/j.ejmech.2020.112767 Plasma 1
32916314 10.1016/j.ejmech.2020.112767 Staphylococcus aureus 1

Data from ChEMBL 36 via Core Engine