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Compound Detail

CHEMBL4279135

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CN(C)CCOc1ccc(-c2cnc3c(-c4ccc(S(N)(=O)=O)c5ccccc45)cnn3c2)cn1

Basic Information

ChEMBL ID CHEMBL4279135
Phase Preclinical
Structure Type MOL
InChI Key NEWWJMLDJTYMCU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

488.6
MW (Da)
3.20
ALogP
8
HBA
1
HBD
115.7
PSA (Ų)
0.37
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N6O3S
MW 488.57
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 5.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activin receptor type-1
CHEMBL5903
IC50 5.99 5.99 1026.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1567 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Activin receptor type-1 IC50 = 1026.0 nM 5.99 Inhibition of ALK2 (unknown origin) using Ulight topo IIa (Thr 1342) peptide as ... 30227946

Literature References

PubMed DOI Target Context # Activities
30227946 10.1016/j.bmcl.2018.09.006 No relevant target 2
30227946 10.1016/j.bmcl.2018.09.006 Activin receptor type-1 1
30227946 10.1016/j.bmcl.2018.09.006 Bone morphogenetic protein receptor type-1A 1
30227946 10.1016/j.bmcl.2018.09.006 ADMET 1

Data from ChEMBL 36 via Core Engine