BRD2 inhibitor II 20μM R07 exp341 [The Human Chemical-Genetic Interaction Map Project]

Inhibits BRD2, blocks recognition of acetylated H4K12

Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor

Compound References

PubChem Name: 1-[2-(1H-Benzimidazol-2-ylsulfanyl)ethyl]-3-methyl-1,3-dihydro-2H-benzimidazole-2-thione
Synonyms: N/A
CAS #: 433249-32-2
PubChem CID: 672548
IUPAC: 1-[2-(1H-benzimidazol-2-ylsulfanyl)ethyl]-3-methylbenzimidazole-2-thione
INCHI Name: InChI=1S/C17H16N4S2/c1-20-14-8-4-5-9-15(14)21(17(20)22)10-11-23-16-18-12-6-2-3-7-13(12)19-16/h2-9H,10-11H2,1H3,(H,18,19)
INCHI Key: KDPSGIFCBZTBEZ-UHFFFAOYSA-N
Molecular Weight: 340.5
Canonical SMILES: CN1C2=CC=CC=C2N(C1=S)CCSC3=NC4=CC=CC=C4N3
Isomeric SMILES: N/A
Molecular Formula: C17H16N4S2

Compound Supplier

Supplier Name: Calbiochem
Catalog #: 203830
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C17H16N4S2 341.08891; found 341.09007

Dose Response Curve

Platform ID: BRD2_inhibitor_II
Min: -10.0210; Max: 25.0673

IC	Concentration (µM)
IC10	N/A
IC20	N/A
IC30	N/A
IC40	N/A
IC50	N/A
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 07
Dose: 20µM
Days of incubation: 8
Doublings: 6.7
Numbers of reads: 18711037

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
3/0	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
KDSR	-3.62	<0.01
FLVCR1	-3.31	<0.01
DKC1	-2.69	0.47
CEPT1	-2.69	0.04
SLC5A3	-2.61	0.05
MRPS33	-2.44	0.15
SCAP	-2.40	0.13
PCYT1A	-2.38	0.13
PLEKHA3	-2.31	0.27
TSPEAR	-2.30	0.15
RTCB	-2.23	0.35
NAE1	-2.21	0.35
ZIC5	-2.21	0.35
TBCD	-2.15	0.39
GYPE	-2.09	0.56
SSB	-2.07	0.35
DHX30	-2.05	0.49
LEO1	-2.03	0.39
WFDC8	-2.01	0.40
ATP5J	-1.97	0.47
PPIP5K2	-1.96	0.47
PHYKPL	-1.96	0.47
CEP57	-1.96	0.47
ESX1	-1.95	0.47
ZNF813	-1.95	0.47
FOXE3	-1.94	0.47
NOC3L	-1.93	0.69
OR11H4	-1.93	0.47
ZNF117	-1.92	0.49
EHF	-1.91	0.47
THOC2	1.88	0.66
DBNDD2	1.88	0.66
DTX3	1.92	0.66
IL18RAP	1.95	0.66
TSR2	1.97	0.75
INTS5	1.99	0.66
PSMC5	1.99	0.66
SLFN5	2.02	0.66
DDX47	2.02	0.66
CROCC	2.03	0.66
CKAP5	2.04	0.66
USP16	2.06	0.66
EBNA1BP2	2.07	0.66
NUP160	2.08	0.66
DOCK6	2.09	0.66
PDS5B	2.11	0.62
MCM7	2.12	0.66
CDC73	2.13	0.66
NUP205	2.14	0.66
MDN1	2.20	0.66
ZNF101	2.22	0.53
TRA2B	2.22	0.66
NHSL1	2.22	0.62
STIL	2.28	0.62
SOCS3	2.40	0.53
PELP1	2.43	0.66
PLRG1	2.47	0.53
NOP16	2.53	0.66
HOXC13	2.54	0.32
POLR2L	2.96	0.66

Screen	Correlation	Plot
Lenalidomide 20μM R07 exp375	0.076	View
Prochlorperazine 5.2μM R02 exp77	0.066	View
SB203580 25μM R03 exp149	0.06	View
Cyclosporin-A 3μM R07 exp348	0.06	View
UNC1999 2μM R03 exp155	0.057	View
ZLN024 50μM R08 exp538	0.054	View
Lapatinib 5μM R01 exp47	0.053	View
CCT251545 20μM R07 exp326	0.053	View
Asunaprenir 3μM R07 exp336	0.053	View

Last modified: 2026/01/15 21:36
by 127.0.0.1