Drug Information

Drug (ID: DG01648) and It's Reported Resistant Information

Name	GSK321
Synonyms	GSK321; (R)-1-(4-fluorobenzyl)-N-(3-((S)-1-hydroxyethyl)phenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3-carboxamide; 1816331-63-1; (7r)-1-(4-Fluorobenzyl)-N-{3-[(1s)-1-Hydroxyethyl]phenyl}-7-Methyl-5-(1h-Pyrrol-2-Ylcarbonyl)-4,5,6,7-Tetrahydro-1h-Pyrazolo[4,3-C]pyridine-3-Carboxamide; CHEMBL4215717; SCHEMBL20067448; GSK-321; BDBM195601; Q27455571; (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; 59D Click to Show/Hide
Structure
Target	.	NOUNIPROTAC	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	6
IsoSMILES	C[C@@H]1CN(CC2=C1N(N=C2C(=O)NC3=CC=CC(=C3)[C@H](C)O)CC4=CC=C(C=C4)F)C(=O)C5=CC=CN5
InChI	InChI=1S/C28H28FN5O3/c1-17-14-33(28(37)24-7-4-12-30-24)16-23-25(27(36)31-22-6-3-5-20(13-22)18(2)35)32-34(26(17)23)15-19-8-10-21(29)11-9-19/h3-13,17-18,30,35H,14-16H2,1-2H3,(H,31,36)/t17-,18+/m1/s1
InChIKey	IVFDDVKCCBDPQZ-MSOLQXFVSA-N
PubChem CID	91864709

Type(s) of Resistant Mechanism of This Drug

ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Click to Show/Hide the Resistance Disease of This Class

Acute myeloid leukemia [ICD-11: 2A60]

Click to Show/Hide

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)			Click to Show/Hide
Key Molecule: Oxalosuccinate decarboxylase (IDH1)				[1]
Molecule Alteration	Missense mutation		p.R132C (c.394C>T)	Molecule Info
Sensitive Disease	Acute myeloid leukemia [ICD-11: 2A60.0]			Disease Info
Experimental Note	Identified from the Human Clinical Data
In Vitro Model	HT-1080 cells	Acetabulum	Homo sapiens (Human)	CVCL_0317
In Vivo Model	Male CD-1 xenograft mouse model			Mus musculus
Experiment for Molecule Alteration	Western blotting analysis
Experiment for Drug Resistance	Diaphorase/resazurin coupled assay; Colony formation assay

References

Ref 1	New IDH1 mutant inhibitors for treatment of acute myeloid leukemiaNat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5.