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Compound Detail

CHEMBL5202492

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O=c1[nH]c2ccccc2nc1/C=C/c1ccccc1Br

Basic Information

ChEMBL ID CHEMBL5202492
Phase Preclinical
Structure Type MOL
InChI Key WRGLRCQOQDVMSQ-MDZDMXLPSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

327.2
MW (Da)
3.86
ALogP
2
HBA
1
HBD
45.8
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11BrN2O
MW 327.18
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.85

Activity Summary

IC50 7 meas. best 5.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B16-F10
CHEMBL612656
IC50 5.12 5.12 7610.0 1
NCI-H460
CHEMBL396
IC50 5.02 5.02 9620.0 1
HCT-116
CHEMBL394
IC50 4.91 4.91 12340.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 4.6 4.6 25320.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 4.17 4.17 66890.0 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 4.11 4.11 77680.0 1
L02
CHEMBL4296457
IC50 4.1 4.1 78980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34998058 10.1016/j.ejmech.2021.114085 Fibroblast growth factor receptor 1 1
34998058 10.1016/j.ejmech.2021.114085 Receptor-type tyrosine-protein kinase FLT3 1
34998058 10.1016/j.ejmech.2021.114085 Fibroblast growth factor receptor 2 1
34998058 10.1016/j.ejmech.2021.114085 Fibroblast growth factor receptor 3 1
34998058 10.1016/j.ejmech.2021.114085 Platelet-derived growth factor receptor beta 1
34998058 10.1016/j.ejmech.2021.114085 Epidermal growth factor receptor 1
34998058 10.1016/j.ejmech.2021.114085 HeLa 229 1
34998058 10.1016/j.ejmech.2021.114085 NCI-H460 1
34998058 10.1016/j.ejmech.2021.114085 HCT-116 1
34998058 10.1016/j.ejmech.2021.114085 B16-F10 1
34998058 10.1016/j.ejmech.2021.114085 L02 1

Data from ChEMBL 36 via Core Engine