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Compound Detail

CHEMBL4802038

A-446
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O=C(Cc1ccccc1)Nc1nnc(N2C[C@H]3C[C@@H]2CN3c2cccnn2)s1

Basic Information

ChEMBL ID CHEMBL4802038
Name A-446
Phase Preclinical
Structure Type MOL
InChI Key DLNFTRSEHUWEGO-HUUCEWRRSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
1.98
ALogP
8
HBA
1
HBD
87.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C19H19N7OS
MW 393.48
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.64

Activity Summary

IC50 2 meas. best 7.98
Ki 2 meas. best 5.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A549
CHEMBL392
IC50 7.98 7.98 10.5 1
Glutaminase kidney isoform, mitochondrial
CHEMBL2146302
IC50 7.51 7.51 31.0 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 5.19 5.19 6453.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A549 IC50 = 10.5 nM 7.98 A549 CTG Assay -
Glutaminase kidney isoform, mitochondrial IC50 = 31.0 nM 7.51 GLS Enzyme activity assay -
5-hydroxytryptamine receptor 1D Ki = 6453.57 nM 5.19 GPCRScan assay: inhibition of 5-HT1D -
5-hydroxytryptamine receptor 1D Ki = 6456.54 nM 5.19 GPCRScan assay: inhibition of 5-HT1D -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 U2OS 10
- 10.6019/CHEMBL5303304 Fibroblast 9
- 10.6019/CHEMBL5303304 HEK-293T 8
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 1D 5
- 10.6019/CHEMBL4800721 Unchecked 3
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 7 3
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 2C 1
- 10.6019/CHEMBL4800721 Alpha-2A adrenergic receptor 1
- 10.6019/CHEMBL4800721 Alpha-1D adrenergic receptor 1
- 10.6019/CHEMBL5665443 Uracil-DNA glycosylase 1
- 10.6019/CHEMBL4800721 Alpha-1A adrenergic receptor 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 6 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 5A 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 3A 1
- 10.6019/CHEMBL4800721 Glutaminase kidney isoform, mitochondrial 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 2B 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 2A 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 1E 1
- 10.6019/CHEMBL4800721 5-hydroxytryptamine receptor 1A 1
- 10.6019/CHEMBL4800721 A549 1

Data from ChEMBL 36 via Core Engine