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Compound Detail

CHEMBL401570

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Cc1cccc(-c2[nH]c(C(C)(C)C)nc2-c2ccc3nccnc3c2)n1

Basic Information

ChEMBL ID CHEMBL401570
Phase Preclinical
Structure Type MOL
InChI Key DKPQHFZUICCZHF-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

343.4
MW (Da)
4.69
ALogP
4
HBA
1
HBD
67.3
PSA (Ų)
0.57
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N5
MW 343.43
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.10

Activity Summary

IC50 4 meas. best 7.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 7.84 7.49 14.3 3
Transforming growth factor beta-1 proprotein/Mothers against decapentaplegic homolog 3
CHEMBL4296078
IC50 7.15 7.15 70.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39018123 10.1021/acs.jmedchem.4c01183 U2OS 12
20472445 10.1016/j.bmc.2010.04.071 TGF-beta receptor type-1 5
18262787 10.1016/j.bmcl.2008.01.084 TGF-beta receptor type-1 3
20621731 10.1016/j.bmcl.2010.05.032 TGF-beta receptor type-1 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
39018123 10.1021/acs.jmedchem.4c01183 Unchecked 2
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
31606345 10.1016/j.bmcl.2019.126695 Unchecked 1
31606345 10.1016/j.bmcl.2019.126695 Transforming growth factor beta-1 proprotein/Mothers against decapentaplegic homolog 3 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
34531950 10.1021/acsmedchemlett.1c00198 Mus musculus 1
32092587 10.1016/j.ejmech.2020.112154 TGF-beta receptor type-1 1
38626523 10.1016/j.ejmech.2024.116395 TGF-beta receptor type-1 1

Data from ChEMBL 36 via Core Engine