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Compound Detail

CHEMBL182066

RADIPRODIL
🧪 Phase II
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🧪 Phase II
O=C(Nc1ccc2nc(O)oc2c1)C(=O)N1CCC(Cc2ccc(F)cc2)CC1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL182066
Name RADIPRODIL
Phase Phase II
Structure Type MOL
InChI Key GKGRZLGAQZPEHO-UHFFFAOYSA-N

Known Names

Radiprodil Rgh-896
4
Targets
9
Activities
1
Assay Types
4
PK Parameters
17
Publications
2
Known Names
2
Indications
1
Mechanisms

Molecular Properties

397.4
MW (Da)
3.09
ALogP
5
HBA
2
HBD
95.7
PSA (Ų)
0.66
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -dil

Extended Properties

Molecular Formula C21H20FN3O4
MW 397.41
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.68

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Glutamate NMDA receptor; GRIN1/GRIN2B antagonist ANTAGONIST Glutamate NMDA receptor; GRIN1/GRIN2B ✓ ✓

Indications

Neuralgia Spasms, Infantile

Activity Summary

IC50 9 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 2B
CHEMBL3442
 IC50 8.5 8.5 3.2 2
Glutamate NMDA receptor; GRIN1/GRIN2B
CHEMBL1907603
 IC50 8.4 8.045 4.0 4
Glutamate [NMDA] receptor
CHEMBL2094124
 IC50 8.22 8.22 6.0 1
Glutamate receptor ionotropic, NMDA 2B
CHEMBL311
 IC50 7.5 7.5 31.6 2

Pharmacokinetic Data

Parameter Value Units Species
CL 37.1 mL.min-1.kg-1 Rattus norvegicus
CL 37.1 mL.min-1.kg-1 Rattus norvegicus
F 30.0 % Rattus norvegicus
F 30.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate receptor ionotropic, NMDA 2B IC50 = 3.162 nM 8.5 Antagonist activity at mouse NR2B expressed in Hek293 cells co-expressing mouse ... 28754363
Glutamate receptor ionotropic, NMDA 2B IC50 = 3.162 nM 8.5 Antagonist activity at mouse NR2B receptor expressed in HEK293 cells co-expressi... 30833109
Glutamate NMDA receptor; GRIN1/GRIN2B IC50 = 4.0 nM 8.4 Inhibition of NMDA-evoked increased intracellular [Ca2+] in cells expressing NR1... 15225705
Glutamate NMDA receptor; GRIN1/GRIN2B IC50 = 4.0 nM 8.4 Antagonist activity against NR1/NR2B receptor 21453995
Glutamate [NMDA] receptor IC50 = 6.0 nM 8.22 Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor 15225705
Glutamate NMDA receptor; GRIN1/GRIN2B IC50 = 6.0 nM 8.22 Displacement of [3H]-Ro-256981 from recombinant NR1/NR2B receptor 21453995
Glutamate receptor ionotropic, NMDA 2B IC50 = 31.62 nM 7.5 Displacement of [3H]-ifenprodil from NR2B in Wistar rat brain membrane after 120... 28754363
Glutamate receptor ionotropic, NMDA 2B IC50 = 31.62 nM 7.5 Displacement of [3H]-ifenprodil from NR2B receptor in rat brain cerebral cortex ... 30833109
Glutamate NMDA receptor; GRIN1/GRIN2B IC50 = 69.91 nM 7.16 Antagonist activity against NR1a/NR2B receptor transfected in human HEK293 cells... 21453995

Literature References

PubMed DOI Target Context # Activities
21453995 10.1016/j.ejmech.2011.03.013 Glutamate NMDA receptor; GRIN1/GRIN2B 3
28754363 10.1016/j.bmcl.2017.06.076 Rattus norvegicus 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
30833109 10.1016/j.bmcl.2019.02.017 ADMET 2
30833109 10.1016/j.bmcl.2019.02.017 Glutamate receptor ionotropic, NMDA 2B 2
28754363 10.1016/j.bmcl.2017.06.076 Glutamate receptor ionotropic, NMDA 2B 2
21453995 10.1016/j.ejmech.2011.03.013 Liver 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
30833109 10.1016/j.bmcl.2019.02.017 Rattus norvegicus 1
28754363 10.1016/j.bmcl.2017.06.076 Voltage-gated inwardly rectifying potassium channel KCNH2 1
15225705 10.1016/j.bmcl.2004.05.053 Glutamate [NMDA] receptor 1
21453995 10.1016/j.ejmech.2011.03.013 Plasma 1
21453995 10.1016/j.ejmech.2011.03.013 Glutamate NMDA receptor; GRIN1/GRIN2A 1
21453995 10.1016/j.ejmech.2011.03.013 Mus musculus 1
15225705 10.1016/j.bmcl.2004.05.053 Mus musculus 1
15225705 10.1016/j.bmcl.2004.05.053 Glutamate NMDA receptor; GRIN1/GRIN2A 1
15225705 10.1016/j.bmcl.2004.05.053 Glutamate NMDA receptor; GRIN1/GRIN2B 1

Data from ChEMBL 36 via Core Engine