BI-D1870 3.15μM R02 exp66 [The Human Chemical-Genetic Interaction Map Project]

Inhibits ribosomal p90 S6 Kinase, active against RSK1/2/3/4 isoforms

Class / Subclass 1: Signal Transduction / Kinase Inhibitor

Compound References

PubChem Name: 2-((3,5-Difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one
Synonyms: N/A
CAS #: 501437-28-1
PubChem CID: 25023738
IUPAC: 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
INCHI Name: InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
INCHI Key: DTEKTGDVSARYDS-UHFFFAOYSA-N
Molecular Weight: 391.4
Canonical SMILES: CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
Isomeric SMILES: N/A
Molecular Formula: C19H23F2N5O2

Compound Supplier

Supplier Name: Selleck Chemicals
Catalog #: S2843
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C19H23F2N5O2 392.18926; found 392.19055

Dose Response Curve

Platform ID: BI-D1870
Min: -18.9777; Max: 94.2694

IC	Concentration (µM)
IC10	N/A
IC20	2.5715
IC30	2.6985
IC40	2.8073
IC50	2.9110
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 02
Dose: 3.15µM
Days of incubation: 8
Doublings: 1.0
Numbers of reads: 9502251

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
2/29	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
ELAVL1	-2.79	0.05
PDS5B	-2.73	0.05
JOSD1	-2.65	0.12
SREK1	-2.56	0.12
CENPL	-2.50	0.15
TMEM230	-2.44	0.12
ARID4B	-2.44	0.12
CDC45	-2.43	0.53
CNOT2	-2.40	0.12
ETFB	-2.38	0.12
CYP1A1	-2.37	0.12
SKA3	-2.37	0.13
RBM15	-2.34	0.12
PRKAA1	-2.33	0.12
BORA	-2.32	0.15
TK1	-2.26	0.12
B4GALT6	-2.26	0.16
TSC2	-2.26	0.12
INTS3	-2.23	0.35
MASTL	-2.19	0.31
COPS3	-2.18	0.15
FNTB	-2.17	0.15
CFAP45	-2.15	0.53
CENPF	-2.15	0.33
TCHP	-2.14	0.33
TUBGCP6	-2.14	0.25
ABHD17B	-2.14	0.16
CCNA2	-2.13	0.33
OR6T1	-2.13	0.16
ATP6AP1	-2.13	0.54
GFM2	2.34	0.04
POLG	2.35	0.06
AASDHPPT	2.39	0.03
PET117	2.39	0.03
PQBP1	2.40	0.03
SNRPB2	2.42	0.03
HSD17B10	2.43	0.04
SSBP1	2.48	0.04
KCTD5	2.49	0.04
NDUFAF3	2.51	0.06
CCNK	2.53	0.02
EIF4A1	2.53	0.03
NDUFB11	2.60	0.03
HIST1H1D	2.61	0.01
KDM1A	2.62	0.04
RB1	2.65	0.02
SPOP	2.73	<0.01
NFU1	2.74	0.03
PUS3	2.77	0.01
RCOR1	2.78	<0.01
CMAS	2.82	<0.01
DDX5	2.84	<0.01
HIST1H1B	2.91	<0.01
DAZAP1	3.11	<0.01
TLK2	3.21	<0.01
CDK10	3.35	<0.01
PGM3	3.42	<0.01
ENY2	3.57	<0.01
TTC14	6.05	<0.01
FAM58A	6.20	<0.01

Screen	Correlation	Plot
UM0125461 0.74μM R02 exp84	0.062	View
Thimerosal 0.85μM R08 exp529	0.062	View
Genistein 15μM R07 exp360	0.06	View
Hydroxyurea 100μM R07 exp329	0.06	View
PU-H71 1μM R08 exp515	0.056	View
UM0129480 7μM R02 exp85	0.055	View
LLY-283 2.6μM R06 exp290	0.052	View
RO-3307 4.7μM R02 exp80	0.051	View
GSK626616 14μM R08 exp485	0.051	View
I-BRD9 4μM R07 exp365	0.051	View
Actinomycin-D 0.001μM R00 exp3	0.056	View

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