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Compound Detail

CHEMBL1916036

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FC(F)(F)c1n[nH]c(-c2nc(Cc3cncnc3)c3ccccn23)n1

Basic Information

ChEMBL ID CHEMBL1916036
Phase Preclinical
Structure Type MOL
InChI Key WVHZOVWSYVTAJO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
8
Publications
0
Known Names

Molecular Properties

345.3
MW (Da)
2.52
ALogP
6
HBA
1
HBD
84.7
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H10F3N7
MW 345.29
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.49

Activity Summary

IC50 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.22 7.22 60.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.0 mL.min-1.g-1 Homo sapiens
CL 16.0 mL.min-1.g-1 Rattus norvegicus
CL 9.9 mL.min-1.kg-1 Rattus norvegicus
F 61.0 % Rattus norvegicus
T1/2 4.1 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 60.0 nM 7.22 Activation of soluble guanylate cyclase in Sprague-Dawley rat thoracic aorta rin... 21924901

Literature References

PubMed DOI Target Context # Activities
21924901 10.1016/j.bmcl.2011.08.071 Rattus norvegicus 4
21924901 10.1016/j.bmcl.2011.08.071 Soluble guanylate cyclase 2
21924901 10.1016/j.bmcl.2011.08.071 Liver microsomes 2
21924901 10.1016/j.bmcl.2011.08.071 Unchecked 1
21924901 10.1016/j.bmcl.2011.08.071 No relevant target 1
21924901 10.1016/j.bmcl.2011.08.071 ADMET 1
21924901 10.1016/j.bmcl.2011.08.071 Cytochrome P450 1A2 1
21924901 10.1016/j.bmcl.2011.08.071 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine