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Compound Detail

CHEMBL1170377

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Cc1cccc(-c2nn(C(=S)Nc3ccccc3)cc2-c2ccnc3ccccc23)n1

Basic Information

ChEMBL ID CHEMBL1170377
Phase Preclinical
Structure Type MOL
InChI Key HIJMSZGHKQPPJS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
5.71
ALogP
5
HBA
1
HBD
55.6
PSA (Ų)
0.38
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H19N5S
MW 421.53
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 7.92 7.92 12.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
TGF-beta receptor type-1 IC50 = 12.0 nM 7.92 Inhibition of TbetaR-1 (unknown origin) 32092587
TGF-beta receptor type-1 IC50 = 12.0 nM 7.92 Inhibition of TGFbetaR1 (unknown origin) 38626523

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 U2OS 5
20621731 10.1016/j.bmcl.2010.05.032 TGF-beta receptor type-1 3
- 10.6019/CHEMBL5303304 Fibroblast 3
- 10.1101/2020.04.21.054387 SARS-CoV-2 1
32092587 10.1016/j.ejmech.2020.112154 TGF-beta receptor type-1 1
- 10.6019/CHEMBL5303304 HEK-293T 1
38626523 10.1016/j.ejmech.2024.116395 TGF-beta receptor type-1 1

Data from ChEMBL 36 via Core Engine