BDBM378885 US10266537, Compound 93
SMILES Cc1ccc(NC(=O)c2ccc(C)c(c2)C(F)(F)F)cc1C#Cc1nn([C@H]2CC[C@H](O)CC2)c2ncnc(N)c12
InChI Key InChIKey=YHVHYWYQEFELOW-HZCBDIJESA-N
Data 85 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 48 hits for monomerid = 378885
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of human full length recombinant Src using Cdc2 peptide as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric sc...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated Qpatch electrophysiological assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of human full length recombinant YES using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometri...More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human HCK (230 to 497 residues) using GGMEDIYFEFMGGKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric ...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human full length recombinant LYN using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometri...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of human full length recombinant FYN using Cdc2 peptide as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric sc...More data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Inhibition of human full length recombinant LCK using KVEKIGEGTYGVVYK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric...More data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Inhibition of human full length recombinant BLK M287V mutant using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] ...More data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibition of human recombinant PTK5 (218 to end residues) using GGEEEEYFELVKKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by ...More data for this Ligand-Target Pair
Affinity DataIC50: 121nMAssay Description:Inhibition of human full length recombinant BRK using poly (Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometr...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant ABL (27 to end residues) using EAIYAAPFAKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radio...More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant ABL T315I mutant (27 to end residues) using EAIYAAPFAKKK as substrate incubated for 40 mins in presence of [gamma33P-...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant ARG (38 to end residues) using EAIYAAPFAKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radio...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 15nMAssay Description:Inhibition of human recombinant FLT1 (783 to end residues) using KKKSPGEYVNIEFG as substrate incubated for 40 mins in presence of [gamma33P-ATP] by r...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 32nMAssay Description:Inhibition of human recombinant KDR (790 to end residues) using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P-ATP]...More data for this Ligand-Target Pair
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 65nMAssay Description:Inhibition of human recombinant DDR2 S642A mutant (467 to end residues) using KKSRGDYMTMQIG as substrate incubated for 40 mins in presence of [gamma3...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant RET (658 to end residues) using KKKSPGEYVNIEFG as substrate incubated for 40 mins in presence of [gamma33P-ATP] by ra...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of human recombinant TXK (256 to end residues) using GEEPLYWSFPAKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by ra...More data for this Ligand-Target Pair
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 21nMAssay Description:Inhibition of human full length recombinant BMX using poly (Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometr...More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of human recombinant FGFR1 (456 to 765 residues) using KKKSPGEYVNIEFG as substrate incubated for 40 mins in presence of [gamma33P-ATP] by ...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Inhibition of human recombinant FGFR2 N549H mutant (456 to 770 residues) using GGEEEEYFELVKKKK as substrate incubated for 40 mins in presence of [gam...More data for this Ligand-Target Pair
Affinity DataIC50: 120nMAssay Description:Inhibition of human recombinant FGFR3 (447 to 761 residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] b...More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 165nMAssay Description:Inhibition of human recombinant ERBB2 G778D mutant (676 to end residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [ga...More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-4(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 122nMAssay Description:Inhibition of human recombinant ERBB4 (706 to 991 residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] b...More data for this Ligand-Target Pair
Affinity DataIC50: 651nMAssay Description:Inhibition of human recombinant EGFR (696 to end residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by...More data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibition of human recombinant EGFR T790M mutant (696 to end residues) using GGMEDIYFEFMGGKKK as substrate incubated for 40 mins in presence of [gam...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of human full length recombinant CSK using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometri...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of human recombinant TIE2 Q939H/Q940H mutant (771 to end residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence o...More data for this Ligand-Target Pair
Affinity DataIC50: 116nMAssay Description:Inhibition of human full length recombinant PYK2 using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometr...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 110nMAssay Description:Inhibition of human recombinant B-Raf (416 to end residues) using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P-AT...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 87nMAssay Description:Inhibition of human recombinant B-RAF V600E mutantMore data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 52nMAssay Description:Inhibition of human recombinant c-RAF Y340D/Y341D mutant (306 to end residues) using inactive MEK1 as substrate incubated for 40 mins in presence of ...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 7(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 50nMAssay Description:Inhibition of human recombinant TAK1 (1 to 313 residues) using casein as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric...More data for this Ligand-Target Pair
Affinity DataIC50: 175nMAssay Description:Inhibition of human recombinant ACK1 (1 to 389 residues) using EFPIYDFLPAKKK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radi...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor TYRO3(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 351nMAssay Description:Inhibition of human recombinant RSE (451 to end residues) using KVEKIGEGTYGVVYK as substrate incubated for 40 mins in presence of [gamma33P-ATP] by r...More data for this Ligand-Target Pair
Affinity DataIC50: 342nMAssay Description:Inhibition of human full length recombinant p38alpha using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P-ATP] by r...More data for this Ligand-Target Pair
Affinity DataIC50: 84nMAssay Description:Inhibition of human full length recombinant p38beta using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P-ATP] by ra...More data for this Ligand-Target Pair
Affinity DataIC50: 143nMAssay Description:Inhibition of human recombinant EPHA7 (613 to 909 residues) using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC incubated for 40 mins in presence of [gamma...More data for this Ligand-Target Pair
Affinity DataIC50: 227nMAssay Description:Inhibition of human recombinant EPHA4 (601 to 892 residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] b...More data for this Ligand-Target Pair
Affinity DataIC50: 255nMAssay Description:Inhibition of human recombinant LIMK1 (285 to 638 residues) using cofilin as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiome...More data for this Ligand-Target Pair
Affinity DataIC50: 559nMAssay Description:Inhibition of human full length recombinant RSK1 using KKKNRTLSVA as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiometric sci...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant RSK2 (2 to end residues) using KKKNRTLSVA as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radiome...More data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 1.29E+3nMAssay Description:Inhibition of human recombinant PDGFRalpha (550 to end residues) using poly(Glu, Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-...More data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor beta(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant PDGFRbeta (557 to end residues) using poly(Glu, Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-A...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human full length recombinant ERK2 using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P-ATP] by radio...More data for this Ligand-Target Pair
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant TRKA (440 to end residues) using KKKSPGEYVNIEFG as substrate incubated for 40 mins in presence of [gamma33P-ATP] by r...More data for this Ligand-Target Pair
Affinity DataIC50: 899nMAssay Description:Inhibition of human recombinant TRKB (455 to end residues) using poly(Glu,Tyr)4:1 as substrate incubated for 40 mins in presence of [gamma33P-ATP] by...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
Sichuan University
Curated by ChEMBL
Sichuan University
Curated by ChEMBL
Affinity DataIC50: 30nMAssay Description:Inhibition of Src in human MDA-MB-231 cells assessed as reduction in phosphorylation of Src incubated for 20 hrs by Western blot analysisMore data for this Ligand-Target Pair