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Found 5 hits Enz. Inhib. hit(s) with Target = 'Transcription activator BRG1' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Transcription activator BRG1


(Homo sapiens)
BDBM50443232
PNG
(CHEMBL3086883)
Show SMILES Cc1cc(N=Nc2ccc(cc2)S(=O)(=O)Nc2ccccn2)c(N)cc1O
Show InChI InChI=1S/C18H17N5O3S/c1-12-10-16(15(19)11-17(12)24)22-21-13-5-7-14(8-6-13)27(25,26)23-18-4-2-3-9-20-18/h2-11,24H,19H2,1H3,(H,20,23)
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Article
PubMed
7.97E+3n/an/an/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Displacement of fluorescein-labeled MS239 from recombinant human SMARCA4 bromodomain after 1 hr by fluorescence anisotropy assay


Citation and Details
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Ligand-Target Pair
Transcription activator BRG1


(Homo sapiens)
BDBM50158688
PNG
(CHEMBL3752911)
PDB
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n/an/an/a 89n/an/an/an/an/a



Genentech

Curated by ChEMBL




Citation and Details
More data for this
Ligand-Target Pair
Transcription activator BRG1


(Homo sapiens)
BDBM50148271
PNG
(CHEMBL3769590)
PDB
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n/an/an/a 1.58E+4n/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL




Citation and Details
More data for this
Ligand-Target Pair
Transcription activator BRG1


(Homo sapiens)
BDBM50092310
PNG
(CHEMBL3581661)
Show SMILES COc1cc2c(cc1-c1c(C)noc1C)[nH]c1ccnc(-c3c(C)[nH]nc3C3CC3)c21
Show InChI InChI=1S/C24H23N5O2/c1-11-21(23(28-27-11)14-5-6-14)24-22-15-10-19(30-4)16(20-12(2)29-31-13(20)3)9-18(15)26-17(22)7-8-25-24/h7-10,14,26H,5-6H2,1-4H3,(H,27,28)
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n/an/an/a>1.00E+4n/an/an/an/an/a



University of Michigan

Curated by ChEMBL


Assay Description
Binding affinity to biotinylated BRG1 (59 to 180 amino acid residues) (unknown origin) expressed in Rosetta2 cells by bio-layer interferometry method


Citation and Details
More data for this
Ligand-Target Pair
Transcription activator BRG1


(Homo sapiens)
BDBM50098311
PNG
(CHEMBL3590408)
Show SMILES CN1CC[C@@H](Nc2ncc(-c3cncc(C)c3)c3cc(C)c(=O)[nH]c23)[C@@H](C1)OCC1CCS(=O)(=O)CC1
Show InChI InChI=1/C27H35N5O4S/c1-17-10-20(13-28-12-17)22-14-29-26(25-21(22)11-18(2)27(33)31-25)30-23-4-7-32(3)15-24(23)36-16-19-5-8-37(34,35)9-6-19/h10-14,19,23-24H,4-9,15-16H2,1-3H3,(H,29,30)(H,31,33)/t23-,24-/s2
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n/an/an/a 2.00E+4n/an/an/an/an/a



¿Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany.

Curated by ChEMBL


Assay Description
Binding affinity to SMARCA4 in human HUT78 cells incubated for 45 mins by mass spectrometry based bromosphere chemoproteomic assay


Citation and Details
More data for this
Ligand-Target Pair