ChEMBL ligand: CHEMBL3545311 (Alunbrig, Ap-26113, AP-26113, AP26113, Brigatinib)
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] There should be some charts here, you may need to enable JavaScript!
Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] There should be some charts here, you may need to enable JavaScript!
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] 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
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
GtoPdb	Wild type ALK	-	10.05	pKi	0.09	nM	Ki	Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504]
ChEMBL	Inhibition of human ALK G1202R mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assay	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (2020) 63: 10726-10741 [PMID:32432477]
ChEMBL	Binding affinity to ALK G1202R mutant (unknown origin)	B	8.39	pIC50	4.1	nM	IC50	J Med Chem (2021) 64: 9152-9165 [PMID:34138566]
ChEMBL	Inhibition of human ALK L1196M mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assay	B	8.77	pIC50	1.7	nM	IC50	J Med Chem (2020) 63: 10726-10741 [PMID:32432477]
ChEMBL	Binding affinity to ALK (unknown origin)	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (2021) 64: 9152-9165 [PMID:34138566]
GtoPdb	-	-	9.43	pIC50	0.37	nM	IC50	Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504]; J Med Chem (2016) 59: 4948-64 [PMID:27144831]
ChEMBL	Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hr	B	9.43	pIC50	0.37	nM	IC50	J Med Chem (2016) 59: 4948-4964 [PMID:27144831]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Inhibition of wild type EGFR (unknown origin) measured by ELISA	B	6.58	pIC50	261.3	nM	IC50	ACS Med Chem Lett (2022) 13: 196-202 [PMID:35178175]
ChEMBL	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as protein phosphorylation measured after 2 hrs by ELISA	B	6.69	pIC50	203	nM	IC50	J Med Chem (2021) 64: 13704-13718 [PMID:34491761]
ChEMBL	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	B	6.89	pIC50	130	nM	IC50	J Nat Prod (2019) 82: 3065-3073 [PMID:31718182]
GtoPdb	-	-	6.89	pIC50	129	nM	IC50	Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504]
ChEMBL	Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA	B	7.29	pIC50	50.9	nM	IC50	ACS Med Chem Lett (2018) 9: 1123-1127 [PMID:30429956]
ChEMBL	Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA	B	7.42	pIC50	38.3	nM	IC50	ACS Med Chem Lett (2018) 9: 1123-1127 [PMID:30429956]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISA	B	7.42	pIC50	38.3	nM	IC50	ACS Med Chem Lett (2022) 13: 196-202 [PMID:35178175]
ChEMBL	Inhibition of Wild type EGFR (unknown origin)	B	7.68	pIC50	21	nM	IC50	J Med Chem (2021) 64: 13704-13718 [PMID:34491761]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay	B	7.73	pIC50	18.5	nM	IC50	Eur J Med Chem (2021) 225: 113786-113786 [PMID:34464874]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme for 3 hrs followed by substrate and ATP addition by TR-FRET assay	B	7.9	pIC50	12.5	nM	IC50	Eur J Med Chem (2021) 225: 113786-113786 [PMID:34464874]
ChEMBL	Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	B	8.52	pIC50	3	nM	IC50	J Med Chem (2019) 62: 7302-7308 [PMID:31298540]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA	B	8.6	pIC50	2.5	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532]
ChEMBL	Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISA	B	8.82	pIC50	1.5	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532]
ChEMBL	Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISA	B	8.82	pIC50	1.5	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532]
ChEMBL	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	B	9	pIC50	1	nM	IC50	J Nat Prod (2019) 82: 3065-3073 [PMID:31718182]
ChEMBL	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	B	9	pIC50	1	nM	IC50	J Nat Prod (2019) 82: 3065-3073 [PMID:31718182]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL	Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr	B	7.6	pIC50	24.9	nM	IC50	J Med Chem (2016) 59: 4948-4964 [PMID:27144831]
GtoPdb	-	-	7.61	pIC50	24.6	nM	IC50	J Med Chem (2016) 59: 4948-64 [PMID:27144831]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL	Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hr	B	6.71	pIC50	196	nM	IC50	J Med Chem (2016) 59: 4948-4964 [PMID:27144831]
GtoPdb	-	-	6.71	pIC50	196	nM	IC50	J Med Chem (2016) 59: 4948-64 [PMID:27144831]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL	Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr	B	8.72	pIC50	1.9	nM	IC50	J Med Chem (2016) 59: 4948-4964 [PMID:27144831]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Inhibition of human FLT3 using EAIYAAPFAKKK as substrate and [gamma-33P]ATP measured after 1 hr	B	8.68	pIC50	2.1	nM	IC50	J Med Chem (2016) 59: 4948-4964 [PMID:27144831]

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]