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Compound Detail

CHEMBL5187454

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Nc1ncnc2c1c(-c1ccc3c(c1)OCO3)cn2[C@H]1CC[C@@H](N)CC1

Basic Information

ChEMBL ID CHEMBL5187454
Phase Preclinical
Structure Type MOL
InChI Key GPFXUGQUULNZPF-BETUJISGSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
2.85
ALogP
7
HBA
2
HBD
101.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21N5O2
MW 351.41
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.19

Activity Summary

IC50 1 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-interacting serine/threonine-protein kinase 2
CHEMBL5014
IC50 9.1 9.1 0.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 12.0 mL.min-1.g-1 Homo sapiens
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35709396 10.1021/acs.jmedchem.2c00604 ADMET 3
38117948 10.1021/acs.jmedchem.3c01039 MDA-MB-231 2
38117948 10.1021/acs.jmedchem.3c01039 HeLa 2
35709396 10.1021/acs.jmedchem.2c00604 Receptor-interacting serine/threonine-protein kinase 2 1
35709396 10.1021/acs.jmedchem.2c00604 Receptor-interacting serine/threonine-protein kinase 1 1
35709396 10.1021/acs.jmedchem.2c00604 Unchecked 1

Data from ChEMBL 36 via Core Engine