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Compound Detail

CHEMBL5559089

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CC(=O)N1CCC(CCn2nc(-c3ccc4[nH]ccc4c3)c3c(N)ncnc32)CC1

Basic Information

ChEMBL ID CHEMBL5559089
Phase Preclinical
Structure Type MOL
InChI Key MHRWDUFPJHUNHX-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

403.5
MW (Da)
3.21
ALogP
6
HBA
2
HBD
105.7
PSA (Ų)
0.54
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N7O
MW 403.49
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 7.32
EC50 1 meas. best 7.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TGF-beta receptor type-1
CHEMBL2021750
EC50 7.53 7.53 29.6 1
TGF-beta receptor type-1
CHEMBL4439
IC50 7.32 7.32 48.3 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.93 4.93 11680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38626523 10.1016/j.ejmech.2024.116395 TGF-beta receptor type-1 3
38626523 10.1016/j.ejmech.2024.116395 4T1 1
38626523 10.1016/j.ejmech.2024.116395 Voltage-gated inwardly rectifying potassium channel KCNH2 1
38626523 10.1016/j.ejmech.2024.116395 L02 1
38626523 10.1016/j.ejmech.2024.116395 HEK-293T 1
38626523 10.1016/j.ejmech.2024.116395 BEAS-2B 1
38626523 10.1016/j.ejmech.2024.116395 MCF-10A 1
38626523 10.1016/j.ejmech.2024.116395 MV4-11 1
38626523 10.1016/j.ejmech.2024.116395 Kasumi 1 1
38626523 10.1016/j.ejmech.2024.116395 U-251 1
38626523 10.1016/j.ejmech.2024.116395 HepG2 1
38626523 10.1016/j.ejmech.2024.116395 MDA-MB-231 1
38626523 10.1016/j.ejmech.2024.116395 PANC-1 1
38626523 10.1016/j.ejmech.2024.116395 Panc02 1
38626523 10.1016/j.ejmech.2024.116395 Vascular endothelial growth factor receptor 2 1
38626523 10.1016/j.ejmech.2024.116395 Epidermal growth factor receptor 1
38626523 10.1016/j.ejmech.2024.116395 Platelet-derived growth factor receptor alpha 1
38626523 10.1016/j.ejmech.2024.116395 Proto-oncogene tyrosine-protein kinase receptor Ret 1
38626523 10.1016/j.ejmech.2024.116395 Serine/threonine-protein kinase B-raf 1
38626523 10.1016/j.ejmech.2024.116395 Tyrosine-protein kinase Lck 1

Data from ChEMBL 36 via Core Engine