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Compound Detail

CHEMBL5549912

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C=CC(=O)N(C)[C@]1(C)C[C@H](Oc2nc(-c3cnn(C)c3)cn3nccc23)C1

Basic Information

ChEMBL ID CHEMBL5549912
Phase Preclinical
Structure Type MOL
InChI Key CRHQQIPBUBMXQQ-DHFPXDALSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

366.4
MW (Da)
2.07
ALogP
7
HBA
0
HBD
77.5
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22N6O2
MW 366.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 9.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.04 9.04 0.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 269.0 mL.min-1.kg-1 Rattus norvegicus
CL 15.0 mL.min-1.kg-1 Homo sapiens
T1/2 15.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.91 nM 9.04 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 5
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