ChEMBL ligand: CHEMBL1078178 (Momelotinib, CYT-387, CYT387, CYT-11387, GS-0387, Cyt-387, CYT-0387)
activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] There should be some charts here, you may need to enable JavaScript!
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] There should be some charts here, you may need to enable JavaScript!
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] Janus kinase 2/Tyrosine-protein kinase JAK2 in Mouse [ChEMBL: CHEMBL1649049] [GtoPdb: 2048] [UniProtKB: Q62120] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	7.6	pKd	25	nM	Kd	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	8.1	pIC50	8	nM	IC50	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	6	pKd	1000	nM	Kd	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	6.39	pIC50	405	nM	IC50	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	7.72	pKd	19	nM	Kd	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	6.97	pIC50	107	nM	IC50	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	6.17	pKd	670	nM	Kd	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
ChEMBL	Biochemical Binding Assay: Biochemical binding assays (DiscoveRx) and in vitro enzyme inhibition assays (LanthaScreen, Life Technologies) were conducted to determine the binding affinity and inhibition activities of CYT-0387 to Type-I BMPR-kinases (ALK2, ALK3, and ALK6) were conducted. Transforming growth factor beta receptor 1 (TGFBR1, ALK5) was used as a control to determine the selectivity to Type-I BMPR-kinases.	B	6.69	pIC50	205	nM	IC50	US-9469613-B2. (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide (2016)
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL	Inhibition of GST-tagged JAK1	B	7.96	pIC50	11	nM	IC50	Bioorg. Med. Chem. Lett. (2009) 19: 5887-5892 [PMID:19762238]
ChEMBL	Inhibition of JAK1 (unknown origin)	B	7.96	pIC50	11	nM	IC50	MedChemComm (2012) 3: 22-27
GtoPdb	-	-	7.96	pIC50	11	nM	IC50	Leukemia (2009) 23: 1441-5 [PMID:19295546]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL	Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP	B	7.39	pIC50	41	nM	IC50	J Med Chem (2018) 61: 6056-6074 [PMID:29940115]
GtoPdb	-	-	7.74	pIC50	18	nM	IC50	Leukemia (2009) 23: 1441-5 [PMID:19295546]
ChEMBL	Inhibition of GST-tagged JAK2 kinase	B	7.74	pIC50	18	nM	IC50	Bioorg. Med. Chem. Lett. (2009) 19: 5887-5892 [PMID:19762238]
ChEMBL	Inhibition of JAK2 V617F mutant (JH1-JH2)	B	7.96	pIC50	11	nM	IC50	Bioorg. Med. Chem. Lett. (2009) 19: 5887-5892 [PMID:19762238]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649049] [GtoPdb: 2048] [UniProtKB: Q62120]
ChEMBL	Inhibition of JAK2 V617F mutant in mouse BAF3 cells	B	5.82	pIC50	1500	nM	IC50	MedChemComm (2012) 3: 22-27
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL	Inhibition of GST-tagged JAK3 kinase	B	6.81	pIC50	155	nM	IC50	Bioorg. Med. Chem. Lett. (2009) 19: 5887-5892 [PMID:19762238]
GtoPdb	-	-	6.81	pIC50	155	nM	IC50	Leukemia (2009) 23: 1441-5 [PMID:19295546]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]