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Compound Detail

CHEMBL272705

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C[C@H](CO)Nc1nc(SCc2ccco2)nc2[nH]c(=O)sc12

Basic Information

ChEMBL ID CHEMBL272705
Phase Preclinical
Structure Type MOL
InChI Key JPKFBTRMHVXMHW-SSDOTTSWSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
2.06
ALogP
8
HBA
3
HBD
104.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H14N4O3S2
MW 338.41
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.50

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
IC50 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 17.0 mL.min-1.kg-1 Rattus norvegicus
CL 8.28 mL.min-1.g-1 Homo sapiens
CL 27.3 uL.min-1.(10^6cells)-1 Homo sapiens
CL 61.0 uL.min-1.(10^6cells)-1 Rattus norvegicus
F 41.0 % Rattus norvegicus
Fu 0.018 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 5
18240390 10.1016/j.bmcl.2007.11.039 Rattus norvegicus 2
18240390 10.1016/j.bmcl.2007.11.039 C-X-C chemokine receptor type 2 1
18240390 10.1016/j.bmcl.2007.11.039 Plasma 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine