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SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2

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Target not currently curated in GtoImmuPdb

Target id: 2739

Nomenclature: SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2

Abbreviated Name: SMARCA2

Family: Non-enzymatic BRD containing proteins

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1590 9p24.3 SMARCA2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Mouse - 1583 19 C1 Smarca2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Rat - 1597 1q51 Smarca2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Previous and Unofficial Names Click here for help
BAF190 | SNF2 | SNF2L2 | SNF2LA | SWI2 | SWI/SNF related
Database Links Click here for help
Alphafold
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GNE-235 Small molecule or natural product Click here for species-specific activity table Hs Binding 5.2 pKd 2
pKd 5.2 (Kd 6x10-6 M) [2]
Description: Binding affinity for hSMARCA2
GNE-064 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.6x10-8 M) [3]
Description: Potency determined by BromoScan assay
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SMD-3040 Small molecule or natural product Click here for species-specific activity table Hs Binding 8.0 pKd 4
pKd 8.0 (Kd 1x10-8 M) [4]
Description: Binding affinity of SMARCA2/4 ligand 3 moiety
A947 Small molecule or natural product Click here for species-specific activity table Hs Binding 7.0 pKd 1
pKd 7.0 (Kd 9.3x10-8 M) [1]
Description: Binding affinity for SMARCA2 bromodomain.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Nicolaides-Baraitser syndrome
Synonyms: Intellectual disability - sparse hair - brachydactyly [Orphanet: ORPHA3051]
OMIM: 601358
Orphanet: ORPHA3051

References

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1. Cantley J, Ye X, Rousseau E, Januario T, Hamman BD, Rose CM, Cheung TK, Hinkle T, Soto L, Quinn C et al.. (2022) Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers. Nat Commun, 13 (1): 6814. [PMID:36357397]

2. Cochran AG, Flynn M. (2023) GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1. J Med Chem, 66 (18): 13116-13134. [PMID:37702400]

3. Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M et al.. (2022) GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. J Med Chem, 65 (16): 11177-11186. [PMID:35930799]

4. Yang L, Tu W, Huang L, Miao B, Kaneshige A, Jiang W, Leng L, Wang M, Wen B, Sun D et al.. (2023) Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong in vivo Antitumor Activity. J Med Chem, 66 (15): 10761-10781. [PMID:37523716]

How to cite this page

Non-enzymatic BRD containing proteins: SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2. Last modified on 18/01/2024. Accessed on 14/06/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2739.