ChEMBL ligand: CHEMBL2336015
discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] There should be some charts here, you may need to enable JavaScript!
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] There should be some charts here, you may need to enable JavaScript!
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] There should be some charts here, you may need to enable JavaScript!
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] 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
discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832]
ChEMBL	Binding affinity to DDR2 (unknown origin) by active-site dependent competition binding assay	B	9.22	pKd	0.6	nM	Kd	J Med Chem (2015) 58: 3287-3301 [PMID:25569119]
ChEMBL	Inhibition of DDR2 (unknown origin) incubated for 1 hr using fluorescein-poly-GAT substrate by TR-FRET based LANCE ULTRA kinase assay	B	6.76	pIC50	175	nM	IC50	J Med Chem (2018) 61: 7977-7990 [PMID:30075624]
GtoPdb	-	-	6.99	pIC50	101.4	nM	IC50	J Med Chem (2013) 56: 3281-95 [PMID:23521020]
ChEMBL	Inhibition of DDR2 (unknown origin) using fluorescein-labeled poly GAT as substrate incubated for 1 hr prior to substrate addition measured after 1 hr by TR-FRET assay	B	6.99	pIC50	101.4	nM	IC50	J Med Chem (2013) 56: 3281-3295 [PMID:23521020]
ChEMBL	Inhibition of recombinant human GST-tagged DDR2 cytoplasmic domain (427 to 855 residues) expressed in baculovirus expression system using Fluorescein-poly GAT as substrate incubated for 1 hr in presence of ATP by LanthaScreen Eu kinase assay	B	6.99	pIC50	101.4	nM	IC50	ACS Med Chem Lett (2020) 11: 379-384 [PMID:32184973]
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
ChEMBL	Binding affinity to DDR1 ATP binding site (unknown origin) after 1 hr by competitive binding assay	B	9.22	pKd	0.6	nM	Kd	J Med Chem (2013) 56: 3281-3295 [PMID:23521020]
ChEMBL	Inhibition of DDR1 (unknown origin) incubated for 1 hr using fluorescein-poly-GAT substrate by TR-FRET based LANCE ULTRA kinase assay	B	8.01	pIC50	9.7	nM	IC50	J Med Chem (2018) 61: 7977-7990 [PMID:30075624]
ChEMBL	Inhibition of DDR1 (unknown origin) using fluorescein-labeled poly GAT as substrate incubated for 1 hr prior to substrate addition measured after 1 hr by TR-FRET assay	B	8.17	pIC50	6.81	nM	IC50	J Med Chem (2013) 56: 3281-3295 [PMID:23521020]
ChEMBL	Inhibition of recombinant human GST-tagged DDR1 catalytic domain (440 to 876 residues) expressed in baculovirus expression system using Fluorescein-poly GAT as substrate incubated for 1 hr in presence of ATP by LanthaScreen Eu kinase assay	B	8.17	pIC50	6.8	nM	IC50	ACS Med Chem Lett (2020) 11: 379-384 [PMID:32184973]
GtoPdb	-	-	8.17	pIC50	6.81	nM	IC50	J Med Chem (2013) 56: 3281-95 [PMID:23521020]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL	Inhibition of c-KIT (unknown origin) using Ser/Thr 6 peptide as substrate incubated for 1 hr prior to substrate addition measured after 2 hrs by FRET assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 3281-3295 [PMID:23521020]
ChEMBL	Inhibition of human recombinant His-tagged c-Kit cytoplasmic domain (544 to 976 residues) expressed in baculovirus expression system using Ser/Thr 6 peptide as substrate after 1 hr in presence of 300 uM ATP by FRET based Z'-LYTE assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2020) 11: 379-384 [PMID:32184973]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL	Inhibition of Abl1 (unknown origin) incubated for 1 hr in presence of Tyrosine-2 peptide substrate by FRET based Z'-Lyte assay	B	6.51	pIC50	308	nM	IC50	J Med Chem (2018) 61: 7977-7990 [PMID:30075624]

ChEMBL data shown on this page come from version 35:

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]