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Compound Detail

CHEMBL502351

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COc1ccc(-c2cnc3c(-c4cccc5ncccc45)cnn3c2)cc1

Basic Information

ChEMBL ID CHEMBL502351
Phase Preclinical
Structure Type MOL
InChI Key FVRYPYDPKSZGNS-UHFFFAOYSA-N
7
Targets
8
Activities
1
Assay Types
6
PK Parameters
20
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
4.62
ALogP
5
HBA
0
HBD
52.3
PSA (Ų)
0.48
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 C22H16N4O
MW 352.40
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.15

Activity Summary

IC50 8 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activin receptor type-1
CHEMBL5903
IC50 7.5 7.5 32.0 2
Activin receptor type-1-like
CHEMBL5311
IC50 7.34 7.34 46.0 1
Bone morphogenetic protein 4
CHEMBL2384894
IC50 6.82 6.82 152.0 1
Bone morphogenetic protein 4
CHEMBL5350
IC50 5.52 5.52 3000.0 1
Bone morphogenetic protein receptor type-1B
CHEMBL5476
IC50 5.01 5.01 9830.0 1
Bone morphogenetic protein receptor type-1A
CHEMBL5275
IC50 4.97 4.97 10800.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 4.71 4.71 19700.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 617.0 mL.min-1.kg-1 Mus musculus
CL 516.0 mL.min-1.kg-1 Homo sapiens
CL 148.0 mL.min-1.kg-1 Rattus norvegicus
Fu 0.014 - Mus musculus
Fu 0.014 - Rattus norvegicus
Fu 0.009 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4495565 SARS-CoV-2 6
- 10.6019/CHEMBL4808148 Histone deacetylase 6 4
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 3
23639540 10.1016/j.bmcl.2013.03.113 Plasma 3
23639540 10.1016/j.bmcl.2013.03.113 Liver microsomes 2
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 2
23639540 10.1016/j.bmcl.2013.03.113 Vascular endothelial growth factor receptor 2 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-1A 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-1B 1
23639540 10.1016/j.bmcl.2013.03.113 Liver 1
18621530 10.1016/j.bmcl.2008.06.052 Bone morphogenetic protein 4 1
23639540 10.1016/j.bmcl.2013.03.113 Unchecked 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein 4 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1-like 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1 1
35108017 10.1021/acs.jmedchem.1c01800 Activin receptor type-1 1
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1B 1
23639540 10.1016/j.bmcl.2013.03.113 TGF-beta receptor type-1 1
23639540 10.1016/j.bmcl.2013.03.113 Bone morphogenetic protein receptor type-2 1
23639540 10.1016/j.bmcl.2013.03.113 TGF-beta receptor type-2 1

Data from ChEMBL 36 via Core Engine