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Compound Detail

CHEMBL353759

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Nc1nc(-c2nn(Cc3ccccc3F)c3ncccc23)ncc1C1CC1

Basic Information

ChEMBL ID CHEMBL353759
Phase Preclinical
Structure Type MOL
InChI Key ATOAHNRJAXSBOR-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
6
PK Parameters
20
Publications
0
Known Names

Molecular Properties

360.4
MW (Da)
3.54
ALogP
6
HBA
1
HBD
82.5
PSA (Ų)
0.60
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 C20H17FN6
MW 360.40
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.62

Activity Summary

IC50 3 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.52 6.52 304.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 45.7 mL.min-1.kg-1 Homo sapiens
CL 101.4 mL.min-1.kg-1 Rattus norvegicus
CL 177.2 mL.min-1.kg-1 Mus musculus
T1/2 0.635 hr Homo sapiens
T1/2 0.4083 hr Rattus norvegicus
T1/2 0.5133 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 304.0 nM 6.52 Activation of rabbit sGC assessed as induction of preconstricted aortic ring rel... 33314936

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 Fibroblast 8
37870434 10.1021/acs.jmedchem.3c01365 Dihydroorotate dehydrogenase (quinone), mitochondrial 6
37870434 10.1021/acs.jmedchem.3c01365 ADMET 6
- 10.6019/CHEMBL5303304 U2OS 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL5303304 HEK-293T 1
- 10.6019/CHEMBL5308504 Peregrin 1
- 10.6019/CHEMBL5308504 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5308504 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5308504 Aurora kinase A 1
- 10.6019/CHEMBL5308504 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5308504 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5308504 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5308504 Casein kinase I isoform delta 1
11277519 10.1016/s0960-894x(01)00073-7 Oryctolagus cuniculus 1
33314936 10.1021/acs.jmedchem.0c01093 Unchecked 1
34106718 10.1021/acs.jnatprod.1c00337 Unchecked 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine