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Compound Detail

CHEMBL5594704

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CC(=O)c1c[nH]c(-c2sc(N(c3cnn(-c4ccncc4F)c3)C3CC3)nc2C(N)=O)c1

Basic Information

ChEMBL ID CHEMBL5594704
Phase Preclinical
Structure Type MOL
InChI Key QCEHAYINFMPPPM-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

451.5
MW (Da)
3.46
ALogP
8
HBA
2
HBD
122.8
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18FN7O2S
MW 451.49
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.44

Activity Summary

IC50 5 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL4439
IC50 8.43 8.43 3.7 1
Activin receptor type-1-like
CHEMBL5311
IC50 7.13 7.13 73.7 1
Activin receptor type-1
CHEMBL5903
IC50 6.74 6.74 183.0 1
Activin receptor type-1B
CHEMBL5310
IC50 5.43 5.43 3690.0 1
Activin receptor type-2B
CHEMBL5466
IC50 5.2 5.2 6344.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38759932 10.1016/j.bmcl.2024.129797 Unchecked 6
38759932 10.1016/j.bmcl.2024.129797 TGF-beta receptor type-1 1
38759932 10.1016/j.bmcl.2024.129797 Activin receptor type-1-like 1
38759932 10.1016/j.bmcl.2024.129797 Activin receptor type-1 1
38759932 10.1016/j.bmcl.2024.129797 Bone morphogenetic protein receptor type-1A 1
38759932 10.1016/j.bmcl.2024.129797 Activin receptor type-1B 1
38759932 10.1016/j.bmcl.2024.129797 Bone morphogenetic protein receptor type-1B 1
38759932 10.1016/j.bmcl.2024.129797 Activin receptor type-2B 1
38759932 10.1016/j.bmcl.2024.129797 Vascular endothelial growth factor receptor 2 1
38759932 10.1016/j.bmcl.2024.129797 Platelet-derived growth factor receptor alpha 1
38759932 10.1016/j.bmcl.2024.129797 High affinity nerve growth factor receptor 1
38759932 10.1016/j.bmcl.2024.129797 Mitogen-activated protein kinase kinase kinase kinase 4 1
38759932 10.1016/j.bmcl.2024.129797 ADMET 1
38759932 10.1016/j.bmcl.2024.129797 No relevant target 1

Data from ChEMBL 36 via Core Engine