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Compound Detail

CHEMBL4069537

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CNC(=O)c1ccc2c(c1)OC[C@H](N1CCc3c(nn(Cc4ccccc4)c3Cl)C1=O)C(=O)N2C

Basic Information

ChEMBL ID CHEMBL4069537
Phase Preclinical
Structure Type MOL
InChI Key CQFIBJVJOHYUIF-IBGZPJMESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

493.9
MW (Da)
2.37
ALogP
6
HBA
1
HBD
96.8
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24ClN5O4
MW 493.95
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.99

Activity Summary

Ki 1 meas. best 9.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-interacting serine/threonine-protein kinase 1
CHEMBL5464
Ki 9.04 9.04 0.9 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.833 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29485864 10.1021/acs.jmedchem.7b01647 Receptor-interacting serine/threonine-protein kinase 1 4
29485864 10.1021/acs.jmedchem.7b01647 Liver 2
29485864 10.1021/acs.jmedchem.7b01647 ADMET 1

Data from ChEMBL 36 via Core Engine