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Compound Detail

CHEMBL2385597

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CC(C)Oc1ccc(-c2cnc3c(-c4ccnc5ccccc45)cnn3c2)cc1

Basic Information

ChEMBL ID CHEMBL2385597
Phase Preclinical
Structure Type MOL
InChI Key JMIFGARJSWXZSH-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
19
Publications
0
Known Names

Molecular Properties

380.4
MW (Da)
5.40
ALogP
5
HBA
0
HBD
52.3
PSA (Ų)
0.42
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N4O
MW 380.45
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.14

Activity Summary

IC50 6 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activin receptor type-1-like
CHEMBL5311
IC50 7.57 7.57 27.0 1
Bone morphogenetic protein receptor type-1B
CHEMBL5476
IC50 7.32 7.32 47.6 1
Activin receptor type-1
CHEMBL5903
IC50 7.0 6.98 100.0 3
Activin receptor type-1B
CHEMBL5310
IC50 5.02 5.02 9622.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 U2OS 5
- 10.6019/CHEMBL5303304 HEK-293T 5
- 10.6019/CHEMBL5303304 Fibroblast 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
23639540 10.1016/j.bmcl.2013.03.113 Activin receptor type-1-like 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
26288266 10.1021/acs.jmedchem.5b00446 Activin receptor type-1 1
26288266 10.1021/acs.jmedchem.5b00446 Unchecked 1
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-1B 1
23639540 10.1016/j.bmcl.2013.03.113 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 Bone morphogenetic protein receptor type-1A 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
23639540 10.1016/j.bmcl.2013.03.113 5'-AMP-activated protein kinase subunit beta-1 1

Data from ChEMBL 36 via Core Engine