Dorsomorphin 5μM R07 exp357

Putative inhibitor of AMPK and BMP signalling

Class / Subclass 1: Signal Transduction / Kinase Inhibitor

Compound References

PubChem Name: Dorsomorphin
Synonyms: BML-275; Compound C
CAS #: 866405-64-3
PubChem CID: 11524144
IUPAC: 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine
INCHI Name: InChI=1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2
INCHI Key: XHBVYDAKJHETMP-UHFFFAOYSA-N
Molecular Weight: 399.5
Canonical SMILES: C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3
Isomeric SMILES: N/A
Molecular Formula: C24H25N5O

Compound Supplier

Supplier Name: Ark Pharm Inc.
Catalog #: AK-88052
Lot #: YF0257195-170620001

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C24H25N5O 400.21319; found 400.21387

Dose Response Curve

Platform ID: Dorsomorphin
Min: 1.3456; Max: 94.1274

IC	Concentration (µM)
IC10	N/A
IC20	1.5365
IC30	2.2301
IC40	3.0231
IC50	4.0073
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 07
Dose: 5µM
Days of incubation: 8
Doublings: 1.0
Numbers of reads: 16049330

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
21/17	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
PRAMEF25	-4.24	0.03
PRAMEF26	-4.20	0.03
BCL2	-3.99	<0.01
RANBP1	-3.54	<0.01
CLK3	-3.28	<0.01
PDS5B	-3.15	<0.01
KIF20A	-3.05	<0.01
ZNF451	-2.96	<0.01
ARL1	-2.93	<0.01
NRAS	-2.86	0.01
ATP6V0A2	-2.77	0.02
LIG4	-2.73	0.02
SCAF1	-2.72	0.22
DCLRE1C	-2.67	0.01
TCF4	-2.65	0.01
PUS7	-2.58	0.03
MAD2L2	-2.57	0.02
PSME3	-2.56	0.02
RRM2B	-2.46	0.03
C1orf68	-2.42	0.03
EDF1	-2.42	0.03
SMG1	-2.39	0.04
OTUB1	-2.36	0.07
HIST1H1B	-2.32	0.05
NELFA	-2.32	0.07
KCNJ2	-2.29	0.06
INCENP	-2.29	0.21
IGLL1	-2.28	0.06
MAD2L1	-2.28	0.06
YPEL5	-2.25	0.06
BRWD1	2.20	0.09
KCTD5	2.21	0.09
SLC7A1	2.22	0.12
C15orf41	2.25	0.07
CYCS	2.28	0.06
MRPL23	2.29	0.06
SART1	2.31	0.35
LARP1	2.33	0.09
TFAP4	2.34	0.05
LOC100505679	2.35	0.44
DGKD	2.41	0.04
EIF4A1	2.42	0.06
OAZ1	2.43	0.04
SMEK1	2.44	0.04
PPA1	2.57	0.07
KLF16	2.64	0.06
EBF1	2.70	0.02
SERF2	2.71	<0.01
SETDB1	2.74	0.04
CRLS1	2.90	<0.01
UBQLN1	3.17	0.00
LCMT1	3.32	0.00
MARCH5	3.39	0.00
APAF1	3.47	0.00
VDAC2	3.48	0.00
PLAA	3.75	0.00
TAZ	4.36	0.00
MLST8	4.92	0.00
BAK1	5.23	0.00
TOP2B	7.21	0.00

Screen	Correlation	Plot
RO-3307 4.7μM R02 exp80	0.09	View
GSK626616 14μM R08 exp485	0.089	View
Milciclib 2μM R08 exp502	0.088	View
Doxorubicin 0.02μM R08 exp478	0.084	View
Hippuristanol 0.12μM R08 exp488	0.084	View
Mitomycin-C 0.06μM R08 exp503	0.083	View
Pyridostatin 4μM R05 exp240	0.083	View
Staurosporine 0.02μM R08 exp524	0.079	View
UM0129480 7μM R02 exp85	0.079	View
Hippuristanol 0.12μM R08 exp489 no dilution day6	0.077	View
JQ1 0.8μM R08 exp435	0.075	View
Etoposide 0.3μM R05 exp199	0.072	View
Quercetin 20μM R08 exp517	0.071	View
Pimelic-diphenylamide-106 5μM R00 exp28	0.071	View
Olaparib 4μM R08 exp512	0.069	View
MS023 7μM R03 exp135	0.069	View
iCRT14 30μM R08 exp492	0.06	View
Hydroxyurea 100μM R07 exp329	0.06	View
SNS-032 15μM R08 exp443	0.058	View
PU-H71 1μM R08 exp515	0.056	View
Wortmannin 5μM R00 exp38	0.056	View
Genistein 15μM R07 exp360	0.056	View
Thapsigargin 0.005μM R07 exp407	0.055	View
Rotenone 20μM R00 exp34	0.055	View
Tanespimycin 14μM R08 exp527	0.053	View
THZ1 0.06μM R08 exp531	0.052	View
Thimerosal 0.85μM R08 exp529	0.051	View
Aphidicolin 0.4μM R08 exp440	0.085	View
Benzoate 20000μM R08 exp456	0.085	View
Actinomycin-D 0.001μM R00 exp3	0.078	View
6-Thio-2-deoxyguanosine 2μM R06 exp259	0.076	View
CR131-b 0.005μM R08 exp474	0.075	View
Bleomycin 5μM R08 exp459	0.07	View
BVD-523 15μM R02 exp67	0.07	View
Centrinone 0.5μM R07 exp343	0.065	View
∆-9-Tetrahydrocannabinol 30μM R08 exp445	0.062	View
AICAR 240μM R03 exp116	0.059	View
Dinaciclib 0.007μM R07 exp355	0.056	View
BML-284 0.09μM R08 exp460	0.055	View
5-Fluorouracil 20μM R00 exp2	0.054	View
CB-5083 0.4μM R08 exp468	0.053	View
5-Azacytidine 2μM R07 exp330	0.053	View
Cannabidiol 20μM R08 exp466	0.052	View
Bortezomib 0.05μM R00 exp7	0.051	View

GO Term	Fold Change	Genes
regulation of mitotic cell cycle phase transition	11.48	BCL2,MAD2L2,PSME3,RRM2B,INCENP,MAD2L1
DNA damage response	6.88	BCL2,PDS5B,LIG4,DCLRE1C,MAD2L2,RRM2B,SMG1,OTUB1

GO Term	Fold Change	Genes
mitochondrial membrane	7.04	BAK1,VDAC2,MARCHF5,CRLS1,MRPL23,CYCS,ROMO1,MTG2,PMAIP1
mitochondrial envelope	6.61	BAK1,VDAC2,MARCHF5,CRLS1,MRPL23,CYCS,ROMO1,MTG2,PMAIP1

Dorsomorphin 5μM R07 exp357

Mechanism of Action

Technical Notes

Compound References

Compound Supplier

Compound Characterization

Dose Response Curve

Screen Summary

Screen Results