ChEMBL ligand: CHEMBL472620
mitogen-activated protein kinase 13/MAP kinase p38 delta in Human [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264] There should be some charts here, you may need to enable JavaScript!
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14 in Human [GtoPdb: 1499] [UniProtKB: Q16539] 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
mitogen-activated protein kinase 13/MAP kinase p38 delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
ChEMBL	Immobilized Metal Affinity Polarization (IMAP) Assay: The MAPK13 blocking activity of test compounds was determined using an immobilized metal affinity polarization (IMAP) assay containing activated MAPK13, FITC-labeled substrate, and test compound. Full-length 6-His-tagged MAPK13 and constitutively active GST-MKK6 were prepared as described below. Activated MAPK13 was generated in 50 mM Hepes, 10 mM MgCl2 and 1 mM DTT, containing 1 uM MAPK13, 2 uM MKK6 and 50 uM ATP for 1 h at 25° C. MKK6 was removed by incubation with glutathione SEPHAROSE 4B beads (GE Healthcare Biosciences). MAPK13 activation was confirmed by Western blot using anti-phospho-p38-MAPK (T180/Y182) antibody (R& D Systems, Minneapolis, Minn.). IMAP assays were performed in 96-well non-treated half-area black plates or 384-well black plates (Corning Inc., Corning, N.Y.) in a final reaction volume of 20 ul using the linear phase of the rate kinetics. Assay reactions contained 0-100 uM test compound, 5-35 nM (EC80) activated MAPK13, 3 uM.	B	6.21	pIC50	619.5	nM	IC50	US-9187470-B2. Anti-mucus drugs and uses therefor (2015)
GtoPdb	-	-	6.21	pIC50	620	nM	IC50	J Clin Invest (2012) 122: 4555-68 [PMID:23187130]
GtoPdb	Determined using an IMAP-based biochemical assay.	-	7.08	pIC50	82.72	nM	IC50	WO2014015056A2. Anti-mucus drugs and uses therefor (2014)
ChEMBL	Immobilized Metal Affinity Polarization (IMAP) Assay: The MAPK13 blocking activity of test compounds was determined using an immobilized metal affinity polarization (IMAP) assay containing activated MAPK13, FITC-labeled substrate, and test compound. Full-length 6-His-tagged MAPK13 and constitutively active GST-MKK6 were prepared as described below. Activated MAPK13 was generated in 50 mM Hepes, 10 mM MgCl2 and 1 mM DTT, containing 1 uM MAPK13, 2 uM MKK6 and 50 uM ATP for 1 h at 25° C. MKK6 was removed by incubation with glutathione SEPHAROSE 4B beads (GE Healthcare Biosciences). MAPK13 activation was confirmed by Western blot using anti-phospho-p38-MAPK (T180/Y182) antibody (R& D Systems, Minneapolis, Minn.). IMAP assays were performed in 96-well non-treated half-area black plates or 384-well black plates (Corning Inc., Corning, N.Y.) in a final reaction volume of 20 ul using the linear phase of the rate kinetics. Assay reactions contained 0-100 uM test compound, 5-35 nM (EC80) activated MAPK13, 3 uM.	B	7.08	pIC50	82.72	nM	IC50	US-9187470-B2. Anti-mucus drugs and uses therefor (2015)
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL	Inhibition of Raf-1	B	6.1	pIC50	800	nM	IC50	Eur J Med Chem (2009) 44: 1240-1249 [PMID:18947905]
mitogen-activated protein kinase 14 in Human [GtoPdb: 1499] [UniProtKB: Q16539]
GtoPdb	-	-	5.44	pIC50	3600	nM	IC50	J Clin Invest (2012) 122: 4555-68 [PMID:23187130]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]