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Compound Detail

CHEMBL5619514

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Cc1cn(-c2cc(NC(=O)Cc3ccccc3Cl)cc(C(F)(F)F)c2)cn1

Basic Information

ChEMBL ID CHEMBL5619514
Phase Preclinical
Structure Type MOL
InChI Key LKTRQPBMQHSQCD-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

393.8
MW (Da)
5.03
ALogP
3
HBA
1
HBD
46.9
PSA (Ų)
0.68
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H15ClF3N3O
MW 393.80
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -2.13

Activity Summary

EC50 1 meas. best 6.7
Kd 1 meas. best 6.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor subfamily 2 group E member 1
CHEMBL1961788
EC50 6.7 6.7 200.0 1
Nuclear receptor subfamily 2 group E member 1
CHEMBL1961788
Kd 6.44 6.44 360.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.583 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39236094 10.1021/acs.jmedchem.4c01443 Unchecked 22
39236094 10.1021/acs.jmedchem.4c01443 Nuclear receptor subfamily 2 group E member 1 3
39236094 10.1021/acs.jmedchem.4c01443 ADMET 2
39236094 10.1021/acs.jmedchem.4c01443 HEK-293T 1
39236094 10.1021/acs.jmedchem.4c01443 A549 1
39236094 10.1021/acs.jmedchem.4c01443 Nuclear receptor ROR-alpha 1
39236094 10.1021/acs.jmedchem.4c01443 No relevant target 1

Data from ChEMBL 36 via Core Engine