DOI: 10.7270/q2hm5czg
title: BindingDB Entry 50010336: Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

description: Small molecule binding data for protein 3-phosphoinositide-dependent protein kinase 1, 5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1, 5'-AMP-activated protein kinase catalytic subunit alpha-2/subunit beta-1/subunit gamma-1, Activin receptor type-1B, Angiopoietin-1 receptor, Aurora kinase A, Aurora kinase B, Aurora kinase C, BDNF/NT-3 growth factors receptor, Beta-adrenergic receptor kinase 1, Beta-adrenergic receptor kinase 2, CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7, Calcium/calmodulin-dependent protein kinase type 1, Calcium/calmodulin-dependent protein kinase type 1D, Calcium/calmodulin-dependent protein kinase type II subunit alpha, Calcium/calmodulin-dependent protein kinase type II subunit beta, Calcium/calmodulin-dependent protein kinase type II subunit delta, Calcium/calmodulin-dependent protein kinase type IV, Casein kinase I isoform alpha, Casein kinase I isoform delta, Casein kinase I isoform epsilon, Casein kinase I isoform gamma-1, Casein kinase I isoform gamma-2, Casein kinase I isoform gamma-3, Casein kinase II subunit alpha, Casein kinase II subunit alpha', Cyclin-A2/Cyclin-dependent kinase 2, Cyclin-T1/Cyclin-dependent kinase 9, Cyclin-dependent kinase 5 activator 1, Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1, Cytochrome P450 2C9, Cytochrome P450 2D6, Cytochrome P450 3A4, Cytoplasmic tyrosine-protein kinase BMX, DNA-dependent protein kinase catalytic subunit, Death-associated protein kinase 1, Death-associated protein kinase 3, Dual specificity mitogen-activated protein kinase kinase 1, Dual specificity mitogen-activated protein kinase kinase 2, Dual specificity mitogen-activated protein kinase kinase 6, Dual specificity protein kinase CLK1, Dual specificity protein kinase CLK2, Dual specificity protein kinase CLK3, Dual specificity tyrosine-phosphorylation-regulated kinase 1A, Dual specificity tyrosine-phosphorylation-regulated kinase 1B, Dual specificity tyrosine-phosphorylation-regulated kinase 3, Dual specificity tyrosine-phosphorylation-regulated kinase 4, Ephrin type-A receptor 1, Ephrin type-A receptor 2, Ephrin type-A receptor 3, Ephrin type-A receptor 4, Ephrin type-A receptor 5, Ephrin type-A receptor 8, Ephrin type-B receptor 1, Ephrin type-B receptor 2, Ephrin type-B receptor 3, Ephrin type-B receptor 4, Epidermal growth factor receptor, Eukaryotic elongation factor 2 kinase, Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 2, Fibroblast growth factor receptor 3, Fibroblast growth factor receptor 4, Focal adhesion kinase 1, G protein-coupled receptor kinase 4, G protein-coupled receptor kinase 5, G protein-coupled receptor kinase 6, Glycogen synthase kinase-3 alpha, Glycogen synthase kinase-3 beta, Hepatocyte growth factor receptor, High affinity nerve growth factor receptor, Homeodomain-interacting protein kinase 1, Homeodomain-interacting protein kinase 2, Homeodomain-interacting protein kinase 3, Homeodomain-interacting protein kinase 4, Inhibitor of nuclear factor kappa-B kinase subunit alpha, Inhibitor of nuclear factor kappa-B kinase subunit beta, Inhibitor of nuclear factor kappa-B kinase subunit epsilon, Insulin receptor, Insulin receptor-related protein, Insulin-like growth factor 1 receptor, Interleukin-1 receptor-associated kinase 1, Interleukin-1 receptor-associated kinase 4, Leucine-rich repeat serine/threonine-protein kinase 2, Leukocyte tyrosine kinase receptor, MAP kinase-activated protein kinase 3, MAP kinase-activated protein kinase 5, MAP kinase-interacting serine/threonine-protein kinase 1, MAP/microtubule affinity-regulating kinase 3, MAP/microtubule affinity-regulating kinase 4, Macrophage colony-stimulating factor 1 receptor, Macrophage-stimulating protein receptor, Mast/stem cell growth factor receptor Kit, Maternal embryonic leucine zipper kinase, Megakaryocyte-associated tyrosine-protein kinase, Misshapen-like kinase 1, Mitogen-activated protein kinase 1, Mitogen-activated protein kinase 10, Mitogen-activated protein kinase 11, Mitogen-activated protein kinase 12, Mitogen-activated protein kinase 13, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase 3, Mitogen-activated protein kinase 8, Mitogen-activated protein kinase 9, Mitogen-activated protein kinase kinase kinase 8, Mitogen-activated protein kinase kinase kinase 9, Mitogen-activated protein kinase kinase kinase kinase 2, Mitogen-activated protein kinase kinase kinase kinase 4, Mitogen-activated protein kinase kinase kinase kinase 5, Muscle, skeletal receptor tyrosine-protein kinase, Myosin light chain kinase 2, skeletal/cardiac muscle, NT-3 growth factor receptor, NUAK family SNF1-like kinase 1, Non-receptor tyrosine-protein kinase TYK2, Nuclear receptor subfamily 1 group I member 2, PAS domain-containing serine/threonine-protein kinase, Phosphatidylinositol 3-kinase catalytic subunit type 3, Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Phosphatidylinositol 4-kinase alpha, Phosphatidylinositol 4-kinase beta, Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform, Platelet-derived growth factor receptor alpha, Platelet-derived growth factor receptor beta, Potassium voltage-gated channel subfamily H member 2, Protein kinase C alpha type, Protein kinase C beta type, Protein kinase C delta type, Protein kinase C epsilon type, Protein kinase C eta type, Protein kinase C gamma type, Protein kinase C iota type, Protein kinase C theta type, Protein kinase C zeta type, Protein-tyrosine kinase 2-beta, Protein-tyrosine kinase 6, Proto-oncogene tyrosine-protein kinase ROS, Proto-oncogene tyrosine-protein kinase Src, Proto-oncogene tyrosine-protein kinase receptor Ret, RAC-alpha serine/threonine-protein kinase, RAC-beta serine/threonine-protein kinase, RAC-gamma serine/threonine-protein kinase, RAF proto-oncogene serine/threonine-protein kinase, Receptor tyrosine-protein kinase erbB-2, Receptor tyrosine-protein kinase erbB-4, Receptor-type tyrosine-protein kinase FLT3, Rho-associated protein kinase 1, Rho-associated protein kinase 2, Rhodopsin kinase GRK7, Ribosomal protein S6 kinase alpha-1, Ribosomal protein S6 kinase alpha-2, Ribosomal protein S6 kinase alpha-3, Ribosomal protein S6 kinase alpha-4, Ribosomal protein S6 kinase alpha-5, Ribosomal protein S6 kinase alpha-6, Ribosomal protein S6 kinase beta-1, SRC kinase signaling inhibitor 1, SRSF protein kinase 1, SRSF protein kinase 2, SRSF protein kinase 3, Serine/threonine-protein kinase 24, Serine/threonine-protein kinase 25, Serine/threonine-protein kinase 26, Serine/threonine-protein kinase 3, Serine/threonine-protein kinase 4, Serine/threonine-protein kinase B-raf, Serine/threonine-protein kinase BRSK1, Serine/threonine-protein kinase Chk1, Serine/threonine-protein kinase Chk2, Serine/threonine-protein kinase D1, Serine/threonine-protein kinase D2, Serine/threonine-protein kinase D3, Serine/threonine-protein kinase DCLK2, Serine/threonine-protein kinase MARK1, Serine/threonine-protein kinase MARK2, Serine/threonine-protein kinase MRCK alpha, Serine/threonine-protein kinase MRCK beta, Serine/threonine-protein kinase N1, Serine/threonine-protein kinase Nek1, Serine/threonine-protein kinase Nek2, Serine/threonine-protein kinase Nek4, Serine/threonine-protein kinase Nek6, Serine/threonine-protein kinase Nek7, Serine/threonine-protein kinase Nek9, Serine/threonine-protein kinase PAK 1, Serine/threonine-protein kinase PAK 2, Serine/threonine-protein kinase PAK 3, Serine/threonine-protein kinase PAK 4, Serine/threonine-protein kinase PAK 5, Serine/threonine-protein kinase PLK1, Serine/threonine-protein kinase PLK2, Serine/threonine-protein kinase PLK3, Serine/threonine-protein kinase SIK2, Serine/threonine-protein kinase Sgk1, Serine/threonine-protein kinase Sgk2 [61-427], Serine/threonine-protein kinase Sgk3, Serine/threonine-protein kinase TAO2, Serine/threonine-protein kinase TBK1, Serine/threonine-protein kinase haspin, Serine/threonine-protein kinase mTOR, Serine/threonine-protein kinase pim-1, Serine/threonine-protein kinase pim-2, Sodium channel protein type 5 subunit alpha, Sphingosine kinase 1, Sphingosine kinase 2, Testis-specific serine/threonine-protein kinase 1, Testis-specific serine/threonine-protein kinase 2, Tyrosine-protein kinase ABL1, Tyrosine-protein kinase ABL2, Tyrosine-protein kinase BTK, Tyrosine-protein kinase Blk, Tyrosine-protein kinase CSK, Tyrosine-protein kinase FRK, Tyrosine-protein kinase Fer, Tyrosine-protein kinase Fes/Fps, Tyrosine-protein kinase Fgr, Tyrosine-protein kinase Fyn, Tyrosine-protein kinase HCK, Tyrosine-protein kinase ITK/TSK, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, Tyrosine-protein kinase JAK3, Tyrosine-protein kinase Lck, Tyrosine-protein kinase Lyn, Tyrosine-protein kinase Mer, Tyrosine-protein kinase SYK, Tyrosine-protein kinase Srms, Tyrosine-protein kinase TXK, Tyrosine-protein kinase Yes, Tyrosine-protein kinase ZAP-70, Tyrosine-protein kinase receptor TYRO3, Tyrosine-protein kinase receptor UFO, Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 2, Vascular endothelial growth factor receptor 3, Voltage-dependent L-type calcium channel subunit alpha-1C, cAMP-dependent protein kinase catalytic subunit PRKX, cAMP-dependent protein kinase catalytic subunit alpha, cGMP-dependent protein kinase 1, and cGMP-dependent protein kinase 2, Uniprot O00141, O00329, O00418, O00506, O00750, O14757, O14920, O14965, O15111, O15146, O15264, O15530, O43293, O43781, O60285, O60563, O60674, O75116, O75469, O75582, O75676, O75914, O94806, O95819, O96013, O96017, P00519, P00533, P04049, P04626, P04629, P05129, P05771, P06213, P06239, P06241, P06493, P07332, P07333, P07947, P07948, P07949, P08069, P08581, P08631, P08684, P08922, P09619, P09769, P10635, P10721, P11309, P11362, P11712, P12931, P14616, P14635, P15056, P15735, P16234, P16591, P17252, P17612, P17948, P19784, P20248, P21709, P21802, P22455, P22607, P23443, P23458, P24723, P24941, P25098, P27361, P27448, P27986, P28482, P29317, P29320, P29322, P29323, P29376, P29597, P30530, P31749, P31751, P32298, P34947, P35626, P35916, P35968, P36507, P36888, P36896, P41240, P41279, P41743, P42336, P42345, P42356, P42679, P42681, P42684, P42685, P43250, P43403, P43405, P45983, P45984, P48729, P48730, P48736, P49674, P49759, P49760, P49761, P49840, P49841, P50613, P50750, P51451, P51617, P51812, P51813, P51817, P51946, P51948, P51955, P51957, P52333, P52564, P53350, P53355, P53778, P53779, P54619, P54646, P54753, P54756, P54760, P54762, P54764, P68400, P78362, P78368, P78527, P80192, Q00535, Q02156, Q02750, Q02763, Q04759, Q04912, Q05397, Q05513, Q05655, Q06187, Q06418, Q08881, Q12809, Q12851, Q12866, Q13043, Q13131, Q13153, Q13177, Q13188, Q13237, Q13464, Q13554, Q13557, Q13627, Q13882, Q13936, Q13976, Q14012, Q14164, Q14289, Q14524, Q14680, Q15078, Q15139, Q15303, Q15349, Q15418, Q15759, Q16288, Q16512, Q16539, Q16566, Q16620, Q16644, Q16816, Q5S007, Q5VT25, Q7KZI7, Q86Z02, Q8IU85, Q8IW41, Q8N4C8, Q8N568, Q8NE63, Q8NEB9, Q8TD19, Q8TDC3, Q8TDX7, Q8TF76, Q8WTQ7, Q96BR1, Q96GD4, Q96L34, Q96PF2, Q96PY6, Q96RG2, Q96SB4, Q9BUB5, Q9BXA7, Q9BZL6, Q9C0H9, Q9H0K1, Q9H1R3, Q9H2X6, Q9H3Y6, Q9H422, Q9H4B4, Q9HBY8, Q9HC98, Q9HCP0, Q9NR20, Q9NRA0, Q9NWZ3, Q9NYA1, Q9NYY3, Q9P0L2, Q9P1W9, Q9P286, Q9P289, Q9UBF8, Q9UHD2, Q9UK32, Q9UL54, Q9UPE1, Q9UQB9, Q9UQM7, Q9Y243, Q9Y463, Q9Y478, Q9Y4K4, Q9Y5S2, Q9Y6E0, and Q9Y6M4