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Compound Detail

CHEMBL3314490

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S=C1Nc2c(oc3ncccc23)C(c2cccc(OCc3cccnc3)c2)N1

Basic Information

ChEMBL ID CHEMBL3314490
Phase Preclinical
Structure Type MOL
InChI Key PCPHCZCRTIQJOL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

388.4
MW (Da)
4.19
ALogP
5
HBA
2
HBD
72.2
PSA (Ų)
0.51
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 C21H16N4O2S
MW 388.45
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.92

Activity Summary

IC50 2 meas. best 6.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily A member 1
CHEMBL6007
IC50 6.03 6.03 940.0 1
Transient receptor potential cation channel subfamily A member 1
CHEMBL5160
IC50 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 100.0 mL.min-1.g-1 Homo sapiens
CL 40.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24953819 10.1016/j.bmcl.2014.05.069 Transient receptor potential cation channel subfamily A member 1 4
24953819 10.1016/j.bmcl.2014.05.069 No relevant target 2
24953819 10.1016/j.bmcl.2014.05.069 Liver microsome 2
24953819 10.1016/j.bmcl.2014.05.069 ADMET 1

Data from ChEMBL 36 via Core Engine