target,target_id,target_uniprot,target_species,ligand,ligand_id,ligand_species,ligand_pubchem_cid,smiles,inchi,inchikey,type,action,action_comment,endogenous,primary_target,concentration_range,affinity_parameter,affinity_high,affinity_median,affinity_low,original_affinity_units,original_affinity_low_nm,original_affinity_median_nm,original_affinity_high_nm,original_affinity_relation,assay_description,receptor_site,ligand_context,pubmed_id mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,CEP-1347,8173,,9917013,CCSCc1ccc2c(c1)c1c3C(=O)NCc3c3c4c1n2[C@H]1C[C@]([C@](O1)(n4c1c3cc(cc1)CSCC)C)(O)C(=O)OC,"InChI=1S/C33H33N3O5S2/c1-5-42-15-17-7-9-22-19(11-17)26-27-21(14-34-30(27)37)25-20-12-18(16-43-6-2)8-10-23(20)36-29(25)28(26)35(22)24-13-33(39,31(38)40-4)32(36,3)41-24/h7-12,24,39H,5-6,13-16H2,1-4H3,(H,34,37)/t24-,32+,33+/m1/s1",SCMLRESZJCKCTC-KMYQRJGFSA-N,Inhibitor,Inhibition,,,,,pIC50,,6.94,,IC50,,114.0,,=,,,,29863360, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,GNE-3511,9355,,72547959,N#Cc1ccnc(c1)Nc1cc(cc(n1)N1CCC(C1)(F)F)C1CCN(CC1)C1COC1,"InChI=1S/C23H26F2N6O/c24-23(25)4-8-31(15-23)22-11-18(17-2-6-30(7-3-17)19-13-32-14-19)10-21(29-22)28-20-9-16(12-26)1-5-27-20/h1,5,9-11,17,19H,2-4,6-8,13-15H2,(H,27,28,29)",RHFIAUKMKYHHFA-UHFFFAOYSA-N,Inhibitor,Inhibition,,,yes,,pKi,,9.3,,Ki,,0.5,,<,,,,26431428, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,"compound 16d [Tao et al., 2009]",9988,,11305809,Cn1nc2c(c1)c1c3C(=O)NCc3c3c(c1CC2)n(C(C)C)c1c3cc(cc1)Oc1ncccn1,"InChI=1S/C27H24N6O2/c1-14(2)33-21-8-5-15(35-27-28-9-4-10-29-27)11-17(21)23-18-12-30-26(34)24(18)22-16(25(23)33)6-7-20-19(22)13-32(3)31-20/h4-5,8-11,13-14H,6-7,12H2,1-3H3,(H,30,34)",GCRBQBQLMPBGQC-UHFFFAOYSA-N,Inhibitor,Inhibition,,,,,pIC50,,9.0,,IC50,,1.0,,=,,,,, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,compound 11 [PMID: 26431428],9989,,91936970,N#Cc1ccnc(c1)Nc1cc(n(n1)C1CCCC1)C1CCN(CC1)C1COC1,"InChI=1S/C22H28N6O/c23-13-16-5-8-24-21(11-16)25-22-12-20(28(26-22)18-3-1-2-4-18)17-6-9-27(10-7-17)19-14-29-15-19/h5,8,11-12,17-19H,1-4,6-7,9-10,14-15H2,(H,24,25,26)",GMTAOJMPNXLKJI-UHFFFAOYSA-N,Inhibitor,Inhibition,,,yes,,pKi,,7.38,,Ki,,42.0,,=,,,,26431428, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,GNE-8505,9990,,90292687,Nc1ncc(cc1C(F)(F)F)c1nn(c(c1)[C@@H]1[C@@H]2[C@H]1CN(C2)C1COC1)CC1CC1,"InChI=1S/C21H24F3N5O/c22-21(23,24)16-3-12(5-26-20(16)25)17-4-18(29(27-17)6-11-1-2-11)19-14-7-28(8-15(14)19)13-9-30-10-13/h3-5,11,13-15,19H,1-2,6-10H2,(H2,25,26)/t14-,15+,19+",IRPVABHDSJVBNZ-QWHZDKJVSA-N,Inhibitor,Inhibition,,,,,pKi,,9.77,,Ki,,0.17,,=,In a TR-FRET assay measuring inhibition of a N-terminally GST-tagged DLK catalytic domain (amino acids 1-520) construct interaction with MKK4 substrate.,,,, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,GDC-0134,11506,,86298636,FC(Oc1cc(cnc1N)c1cc(nc(n1)N1CCC(C1)(F)F)N1C[C@@H]2C[C@H]1CO2)F,"InChI=1S/C19H20F4N6O2/c20-17(21)31-14-3-10(6-25-16(14)24)13-5-15(29-7-12-4-11(29)8-30-12)27-18(26-13)28-2-1-19(22,23)9-28/h3,5-6,11-12,17H,1-2,4,7-9H2,(H2,24,25)/t11-,12-/m0/s1",SKMKJBYBPYBDMN-RYUDHWBXSA-N,Inhibitor,Inhibition,,,,,pKi,,8.35,,Ki,,4.48,,=,Inhibition of human DLK catalytic domain activity (1 to 520 amino acids) in a TR-FRET assay.,,,, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,IACS-52825,12909,,156274380,NC1=NC=C(C2=CN(C34CC(C3)(F)C4)C([C@@H](O)C(F)(F)F)=N2)C=C1OC(F)(F)F,"InChI=1S/C16H13F7N4O2/c17-13-4-14(5-13,6-13)27-3-8(26-12(27)10(28)15(18,19)20)7-1-9(11(24)25-2-7)29-16(21,22)23/h1-3,10,28H,4-6H2,(H2,24,25)/t10-,13?,14?/m1/s1",XUOJHVFYSAMHNK-GWMXKSKGSA-N,Inhibitor,Inhibition,,,,,pIC50,,6.97,,IC50,,107.0,,=,Inhibition of c-Jun phosphorylation in HEK293 cells stably expressing hDLK,,,37436942, mitogen-activated protein kinase kinase kinase 12,2072,Q12852,Human,IACS-52825,12909,,156274380,NC1=NC=C(C2=CN(C34CC(C3)(F)C4)C([C@@H](O)C(F)(F)F)=N2)C=C1OC(F)(F)F,"InChI=1S/C16H13F7N4O2/c17-13-4-14(5-13,6-13)27-3-8(26-12(27)10(28)15(18,19)20)7-1-9(11(24)25-2-7)29-16(21,22)23/h1-3,10,28H,4-6H2,(H2,24,25)/t10-,13?,14?/m1/s1",XUOJHVFYSAMHNK-GWMXKSKGSA-N,Inhibitor,Inhibition,,,,,pKd,,8.89,,Kd,,1.3,,=,Binding dissociation constant determined in the proprietary KINOMEscan KdELECT system,,,37436942,