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Compound Detail

CHEMBL4096813

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CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2[nH]1

Basic Information

ChEMBL ID CHEMBL4096813
Phase Preclinical
Structure Type MOL
InChI Key RPMGXDCRCWWCRY-JTQLQIEISA-N
4
Targets
12
Activities
3
Assay Types
4
PK Parameters
20
Publications
0
Known Names

Molecular Properties

288.4
MW (Da)
1.54
ALogP
4
HBA
2
HBD
70.2
PSA (Ų)
0.90
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C15H20N4O2
MW 288.35
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -1.04

Activity Summary

IC50 5 meas. best 9.1
Ki 5 meas. best 5.82
EC50 2 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxidized purine nucleoside triphosphate hydrolase
CHEMBL3708265
IC50 9.1 8.732 0.8 5
Oxidized purine nucleoside triphosphate hydrolase
CHEMBL3708265
EC50 8.12 8.12 7.6 2
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.82 5.81 1527.0 2
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 5.82 5.82 1527.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.0 5.0 10000.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 36.0 mL.min-1.g-1 Mus musculus
CL 9.0 mL.min-1.kg-1 Rattus norvegicus
CL 4.833 mL.min-1.kg-1 Homo sapiens
Fu 0.48 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxidized purine nucleoside triphosphate hydrolase IC50 = 0.8 nM 9.1 Inhibition of human full length MTH1 using 8-Oxo-2-dGTP as substrate preincubate... 29485874
Oxidized purine nucleoside triphosphate hydrolase IC50 = 2.3 nM 8.64 Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia c... 32184970
Oxidized purine nucleoside triphosphate hydrolase IC50 = 2.3 nM 8.64 PPiLight Biochemical Assay -
Oxidized purine nucleoside triphosphate hydrolase IC50 = 2.3 nM 8.64 Affinity Biochemical interaction (PPiLight Biochemical Assay (full-length human ... -
Oxidized purine nucleoside triphosphate hydrolase IC50 = 2.3 nM 8.64 Inhibition of N-terminal His-tagged full-length recombinant human MTH1 (1 to 156... 28679043
Oxidized purine nucleoside triphosphate hydrolase EC50 = 7.6 nM 8.12 Cellular Thermal Shift Assay (CETSA) -
Oxidized purine nucleoside triphosphate hydrolase EC50 = 7.6 nM 8.12 Affinity On-target Cellular interaction (CETSA (cellular thermal shift assay in ... -
GABA-A receptor; anion channel Ki = 1527.0 nM 5.82 GPCRScan assay: inhibition of GABAA/BZP -
Gamma-aminobutyric acid receptor subunit alpha-1 Ki = 1527.0 nM 5.82 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000302b GABRA1 -
GABA-A receptor; anion channel Ki = 1584.89 nM 5.8 GPCRScan assay: inhibition of GABAA/BZP -
5-hydroxytryptamine receptor 1A Ki = 10000.0 nM 5.0 GPCRScan assay: inhibition of 5-HT1A -
5-hydroxytryptamine receptor 1A Ki = 10000.0 nM 5.0 GPCRScan assay: inhibition of 5-HT1A -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4689842 HEK-293T 10
28679043 10.1021/acschembio.7b00370 ADMET 9
- 10.6019/CHEMBL4689842 U2OS 9
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507271 Unchecked 8
28679043 10.1021/acschembio.7b00370 Unchecked 6
- 10.6019/CHEMBL4507271 GABA-A receptor; anion channel 4
- 10.6019/CHEMBL4507271 5-hydroxytryptamine receptor 1A 3
28679043 10.1021/acschembio.7b00370 CT26 3
28679043 10.1021/acschembio.7b00370 NCI-H460 3
29485874 10.1021/acs.jmedchem.7b01884 ADMET 3
29485874 10.1021/acs.jmedchem.7b01884 Oxidized purine nucleoside triphosphate hydrolase 2
28679043 10.1021/acschembio.7b00370 MCF7 2
- 10.6019/CHEMBL4507271 Oxidized purine nucleoside triphosphate hydrolase 2
29485874 10.1021/acs.jmedchem.7b01884 Liver 2
28679043 10.1021/acschembio.7b00370 No relevant target 2
28679043 10.1021/acschembio.7b00370 NCI-H358 2
- 10.6019/CHEMBL4507271 5-hydroxytryptamine receptor 1B 1
- 10.6019/CHEMBL4507271 5-hydroxytryptamine receptor 1D 1
- 10.1021/acschembio.2c00877 Colon organoid 1

Data from ChEMBL 36 via Core Engine