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Compound Detail

CHEMBL5550053

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C=CC(=O)N1CC[C@H]2[C@@H](Oc3nc(-c4cnn(C)c4)cn4nccc34)C[C@H]21

Basic Information

ChEMBL ID CHEMBL5550053
Phase Preclinical
Structure Type MOL
InChI Key QARNVRFWIILYHB-XYPHTWIQSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

364.4
MW (Da)
1.68
ALogP
7
HBA
0
HBD
77.5
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N6O2
MW 364.41
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.73

Activity Summary

IC50 1 meas. best 10.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 10.59 10.59 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 70.0 mL.min-1.kg-1 Rattus norvegicus
CL 12.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.026 nM 10.59 Inhibition of CD69 expression on CD19+ B-cells in human whole blood pretreated f... 38712838

Literature References

PubMed DOI Target Context # Activities
38712838 10.1021/acs.jmedchem.4c00220 ADMET 4
38712838 10.1021/acs.jmedchem.4c00220 TMD8 2
38712838 10.1021/acs.jmedchem.4c00220 Tyrosine-protein kinase BTK 1
38712838 10.1021/acs.jmedchem.4c00220 Unchecked 1

Data from ChEMBL 36 via Core Engine