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Compound Detail

CHEMBL5598527

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C=C(c1ccc(F)cc1C(F)(F)F)c1cnc2n1CCN(c1cn[nH]c(=O)c1Cl)C2

Basic Information

ChEMBL ID CHEMBL5598527
Phase Preclinical
Structure Type MOL
InChI Key IBGFODGJEVMWQN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
2
Publications
0
Known Names

Molecular Properties

439.8
MW (Da)
3.86
ALogP
5
HBA
1
HBD
66.8
PSA (Ų)
0.63
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14ClF4N5O
MW 439.80
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.60

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Short transient receptor potential channel 5
CHEMBL1250411
IC50 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 73.0 mL.min-1.g-1 Homo sapiens
CL 607.0 mL.min-1.g-1 Rattus norvegicus
CL 247.0 mL.min-1.g-1 Mus musculus
F 21.2 % Homo sapiens
F 6.82 % Rattus norvegicus
F 15.3 % Mus musculus
T1/2 0.48 hr Homo sapiens
T1/2 0.05767 hr Rattus norvegicus
T1/2 0.142 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38878518 10.1016/j.ejmech.2024.116565 ADMET 9
38878518 10.1016/j.ejmech.2024.116565 Short transient receptor potential channel 5 1

Data from ChEMBL 36 via Core Engine