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!
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] 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	Inhibition of ALK G1202R mutant (unknown origin)	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (2022) 65: 15540-15558 [PMID:36395392]
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 ALK L1196M mutant (unknown origin)	B	8.77	pIC50	1.7	nM	IC50	J Med Chem (2022) 65: 15540-15558 [PMID:36395392]
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 EGFR L858R/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of 1 mM ATP by ADP-Glo reagent based assay	B	5.76	pIC50	1718	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
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 wild type EGFR (unknown origin) by ELISA	B	6.85	pIC50	139.7	nM	IC50	J Med Chem (2022) 65: 6840-6858 [PMID:35446588]
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 wild type EGFR (unknown origin)	B	6.91	pIC50	124	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of wild-type EGFR (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay	B	6.96	pIC50	109	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
ChEMBL	Inhibition of wild type EGFR (unknown origin)	B	7.13	pIC50	74.8	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
ChEMBL	Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay	B	7.28	pIC50	53	nM	IC50	Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687]
ChEMBL	Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay	B	7.28	pIC50	53	nM	IC50	Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)	B	7.28	pIC50	52.93	nM	IC50	Bioorg Med Chem Lett (2024) 101: 129648-129648 [PMID:38331226]
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 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 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 mutant (unknown origin) by ELISA	B	7.42	pIC50	37.6	nM	IC50	J Med Chem (2022) 65: 6840-6858 [PMID:35446588]
ChEMBL	Inhibition of EGFR L858R mutant (unknown origin)	B	7.55	pIC50	28.3	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
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 mutant (unknown origin) by ELISA	B	7.76	pIC50	17.2	nM	IC50	J Med Chem (2022) 65: 6840-6858 [PMID:35446588]
ChEMBL	Inhibition of EGFR L858R mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay	B	7.8	pIC50	16	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
ChEMBL	Inhibition of EGFR L858R mutant (unknown origin)	B	7.85	pIC50	14	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
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 EGFR Del19 mutant (unknown origin)	B	7.92	pIC50	12	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of EGFR L858R/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 20 mins by HTRF assay	B	7.96	pIC50	11	nM	IC50	ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473]
ChEMBL	Inhibition of EGFR del19 mutant (unknown origin)	B	7.98	pIC50	10.5	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in Bac-to-Bac baculovirus expression system measured after 2 hrs by ELISA method	B	8.1	pIC50	8	nM	IC50	Eur J Med Chem (2022) 244: 114856-114856 [PMID:36279692]
ChEMBL	Inhibition of EGFR 19 del/T790M/C797S mutant (unknown origin) by ELISA	B	8.18	pIC50	6.6	nM	IC50	J Med Chem (2022) 65: 6840-6858 [PMID:35446588]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay	B	8.27	pIC50	5.4	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
ChEMBL	Inhibition of EGFR L858R/T790M double mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
ChEMBL	Inhibition of EGFR dTCb mutant (unknown origin)	B	8.3	pIC50	5	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)	B	8.31	pIC50	4.9	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
ChEMBL	Inhibition of EGFR LTb mutant (unknown origin)	B	8.35	pIC50	4.5	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay	B	8.36	pIC50	4.4	nM	IC50	J Med Chem (2023) 66: 14633-14652 [PMID:37885208]
ChEMBL	Inhibition of EGFR LTCb mutant (unknown origin)	B	8.36	pIC50	4.4	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) preincubated for 10 mins followed by ATP and substrate addition and measured after 60 mins by plate reader analysis	B	8.36	pIC50	4.4	nM	IC50	J Med Chem (2023) 66: 6849-6868 [PMID:37141440]
ChEMBL	Inhibition of EGFR del19/T790M/C797S mutant (unknown origin)	B	8.41	pIC50	3.9	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay	B	8.47	pIC50	3.38	nM	IC50	Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687]
ChEMBL	Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay	B	8.47	pIC50	3.38	nM	IC50	Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715]
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 wild type EGFR (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 25 mins by HTRF assay	B	8.8	pIC50	1.6	nM	IC50	ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473]
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 EGFR L858R/T790M/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 10 mins by HTRF assay	B	8.89	pIC50	1.3	nM	IC50	ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473]
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]
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 EGFR Del19/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay	B	9.09	pIC50	0.82	nM	IC50	Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687]
ChEMBL	Inhibition of EGFR del18/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay	B	9.09	pIC50	0.82	nM	IC50	Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715]
ChEMBL	Inhibition of EGFR del19/T790M mutant (unknown origin)	B	9.15	pIC50	0.7	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415]
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]
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
ChEMBL	Inhibition of NUAK1 (unknown origin)	B	7.33	pIC50	47	nM	IC50	J Med Chem (2021) 64: 2-25 [PMID:33356242]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]