Synonyms: GDC 0834
Compound class:
Synthetic organic
Comment: GDC-0834 was identified as a clinical candidate antiinflammatory Bruton's tyrosine kinase (BTK) inhibitor, through SAR guided improvements to the pharmacokinetic (PK) properties of the potent and selective BTK inhibitor CGI1746 [4]. GDC-0834 retains CGI1746's selectivity but exhibits significantly improved PK in preclinical animal models [1]. Studies suggest the involvement of aldehyde oxidase (AO) in the rapid amide hydrolysis of GDC-0834 to an inactive metabolite [3], which severly impacted on its ability to sustain beneficial clinical effects. Significant species difference in AO-induced inactivation of GDC-0834 are reported and explain why this was not picked up during preclinical studies [2]. Clinical development was terminated, with the manufacturer using insight gained to inform their search for improved inhibitors.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Classification ![]() |
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Compound class | Synthetic organic |
IUPAC Name ![]() |
N-[3-[6-[4-[(2R)-1,4-dimethyl-3-oxopiperazin-2-yl]anilino]-4-methyl-5-oxopyrazin-2-yl]-2-methylphenyl]-4,5,6,7-tetrahydro-1-benzothiophene-2-carboxamide |
Synonyms ![]() |
GDC 0834 |
Database Links ![]() |
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BindingDB Ligand | 50388183 |
ChEMBL Ligand | CHEMBL2057915 |
GtoPdb PubChem SID | 315661338 |
PubChem CID | 25234918 |
RCSB PDB Ligand | 2VL |
Search Google for chemical match using the InChIKey | CDOOFZZILLRUQH-GDLZYMKVSA-N |
Search Google for chemicals with the same backbone | CDOOFZZILLRUQH |
SynPHARM | 83743 (in complex with Bruton tyrosine kinase) |
UniChem Compound Search for chemical match using the InChIKey | CDOOFZZILLRUQH-GDLZYMKVSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | CDOOFZZILLRUQH-GDLZYMKVSA-N |