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Compound Detail

CHEMBL4874774

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Cc1ncnc2c1ccn2[C@@H]1O[C@@H]2[C@H](Cc3ccc4cc(Br)c(N)nc4c3)CC[C@]2(O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4874774
Phase Preclinical
Structure Type MOL
InChI Key CHFDOIQYYQBEKE-BNQFTCSMSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

510.4
MW (Da)
3.27
ALogP
8
HBA
3
HBD
119.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24BrN5O3
MW 510.39
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness 0.57

Activity Summary

EC50 1 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Z-138
CHEMBL4483276
EC50 8.85 8.85 1.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 27.0 mL.min-1.kg-1 Rattus norvegicus
CL 2163.0 mL.min-1.kg-1 Rattus norvegicus
F 46.0 % Rattus norvegicus
MRT 1.1 hr Rattus norvegicus
Vd 148.0 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Z-138 EC50 = 1.4 nM 8.85 Antiproliferative activity against human Z138 cells incubated for 10 days by cel... 33755451

Literature References

PubMed DOI Target Context # Activities
33755451 10.1021/acs.jmedchem.0c02083 ADMET 5
33755451 10.1021/acs.jmedchem.0c02083 No relevant target 3
33755451 10.1021/acs.jmedchem.0c02083 Protein arginine N-methyltransferase 5 1
33755451 10.1021/acs.jmedchem.0c02083 Z-138 1

Data from ChEMBL 36 via Core Engine