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Found 438 with Last Name = 'dack' and Initial = 'kn'
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50448785(CHEMBL3128069)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of ROS1 (unknown origin) by Pfizer mobility shift assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGamma-aminobutyric acid receptor subunit alpha-2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM430025(4-(4′-Ethanesulfonyl-6-fluoro-2′-metho...)
Affinity DataKi: <0.600nMAssay Description:The affinity of the test compounds was determined by radioligand competition binding assay, using the known compound [3H]Ro-15-1788 (Flumazenil) (Per...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM430027(5-[5-(1-Ethyl-1H-pyrazolo[3,4-c]pyridazin-4-yl)-2-...)
Affinity DataKi:  11.8nMAssay Description:The affinity of the test compounds was determined by radioligand competition binding assay, using the known compound [3H]Ro-15-1788 (Flumazenil) (Per...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGamma-aminobutyric acid receptor subunit alpha-2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM430026(4-(4′-Ethanesulfonyl-6-fluorobiphenyl-3-yl)-...)
Affinity DataKi:  17.5nMAssay Description:The affinity of the test compounds was determined by radioligand competition binding assay, using the known compound [3H]Ro-15-1788 (Flumazenil) (Per...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344193((S)-2-(1-((S)-1-carboxy-2-(5-phenyloxazol-2-yl)eth...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344195((S)-2-(1-((S)-1-carboxy-2-(5-(4-chlorophenyl)oxazo...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227724(CHEMBL400083 | N-hydroxy-2-methyl-2-{4-[2-methyl-3...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227723(2-{4-[3'-(2-amino-ethoxy)-2-methyl-biphenyl-4-yl]-...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVasopressin V1a receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50354912(CHEMBL1837039)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108204(3-[1-Benzo[1,3]dioxol-5-yl-2-(2-ethoxy-4-methyl-be...)
Affinity DataIC50:  0.550nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50085452((S)-2-[((S)-6-Amino-2-methanesulfonylamino-hexanoy...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
TargetNeprilysin(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344191((S)-2-(1-((S)-1-carboxy-2-(5-phenyloxazol-2-yl)eth...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108202((S)-2-(4,6-Dimethoxy-pyrimidin-2-yloxy)-3-methoxy-...)
Affinity DataIC50:  0.800nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50448785(CHEMBL3128069)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227722(CHEMBL398641 | N-hydroxy-2-{4-[3'-(2-hydroxy-ethox...)
Affinity DataIC50:  1nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227725(2-{4-[3'-(2-dimethylamino-ethoxy)-2-methyl-bipheny...)
Affinity DataIC50:  1nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227709(CHEMBL251917 | N-hydroxy-2-(4-(4-(6-(2-hydroxyetho...)
Affinity DataIC50:  1nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50560311(CHEMBL4756197)
Affinity DataIC50:  1nMAssay Description:Agonist activity at human glucocorticoid receptor in PBMC assessed as inhibition of LPS-induced TNFalpha releaseMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108192(3-[1-Benzo[1,3]dioxol-5-yl-2-(2-methoxy-4-methyl-b...)
Affinity DataIC50:  1.10nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVasopressin V1a receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50354897(CHEMBL1837041)
Affinity DataIC50:  1.30nMAssay Description:Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNatriuretic peptides A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344187((S)-2-((S)-1-((S)-2-(biphenyl-4-yl)-1-carboxyethyl...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of atrial natriuretic peptideMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108194(3-[1-Benzo[1,3]dioxol-5-yl-2-oxo-2-(toluene-4-sulf...)
Affinity DataIC50:  1.80nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344197((S)-2-(1-((S)-1-carboxy-2-(3-phenyl-1,2,4-oxadiazo...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227711(2-[4-(3'-ethoxy-2-methyl-biphenyl-4-yl)-piperidine...)
Affinity DataIC50:  2nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Fer(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50448785(CHEMBL3128069)
Affinity DataIC50:  2nMAssay Description:Inhibition of FER (unknown origin) using Km levels of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeukocyte tyrosine kinase receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50448785(CHEMBL3128069)
Affinity DataIC50:  2nMAssay Description:Inhibition of LTK (unknown origin) using Km levels of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50560326(CHEMBL4758563)
Affinity DataIC50:  2nMAssay Description:Agonist activity at human glucocorticoid receptor in PBMC assessed as inhibition of LPS-induced TNFalpha releaseMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50560315(CHEMBL4763360)
Affinity DataIC50:  2nMAssay Description:Agonist activity at human glucocorticoid receptor in PBMC assessed as inhibition of LPS-induced TNFalpha releaseMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50560313(CHEMBL4762028)
Affinity DataIC50:  2nMAssay Description:Agonist activity at human glucocorticoid receptor in PBMC assessed as inhibition of LPS-induced TNFalpha releaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536220(CHEMBL4528395)
Affinity DataIC50:  2nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108187(3-[1-Benzo[1,3]dioxol-5-yl-2-(4-isopropyl-benzenes...)
Affinity DataIC50:  2.30nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536209(CHEMBL4539949)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536208(CHEMBL4483364)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536217(CHEMBL4517645)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108185(3-[1-Benzo[1,3]dioxol-5-yl-2-(4-methoxy-benzenesul...)
Affinity DataIC50:  2.80nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227717(CHEMBL251916 | N-hydroxy-2-{4-[3'-(2-methoxy-ethox...)
Affinity DataIC50:  3nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVasopressin V1a receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50354913(CHEMBL1837028)
Affinity DataIC50:  3nMAssay Description:Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227728(2-[4-(2-fluoro-biphenyl-4-yl)-3,6-dihydro-2H-pyrid...)
Affinity DataIC50:  3nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227733(CHEMBL255030 | N-hydroxy-2-[4-(3'-methoxymethyl-2-...)
Affinity DataIC50:  3nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108193(2-[2-Benzo[1,3]dioxol-5-yl-2-(6-carbamoyl-1-methyl...)
Affinity DataIC50:  3.10nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536198(CHEMBL4534573)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetVasopressin V1a receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50354895(CHEMBL1837038)
Affinity DataIC50:  3.20nMAssay Description:Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536221(CHEMBL4554460)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536214(CHEMBL4560212)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536200(CHEMBL4483513)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNatriuretic peptides A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50085452((S)-2-[((S)-6-Amino-2-methanesulfonylamino-hexanoy...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of atrial natriuretic peptideMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50108196(3-[1-Benzo[1,3]dioxol-5-yl-2-(4-isopropyl-benzenes...)
Affinity DataIC50:  3.5nMAssay Description:Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536216(CHEMBL4580425)
Affinity DataIC50:  4nMAssay Description:Inhibition of human His-tagged JAK3 expressed in baculovirus using biotin-synthetic peptide as substrate after 20 mins by HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetStromelysin-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50227710(2-[4-(3'-ethoxy-2-methyl-biphenyl-4-yl)-3,6-dihydr...)
Affinity DataIC50:  4nMAssay Description:Inhibition of MMP3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Leo Pharma

Curated by ChEMBL
LigandPNGBDBM50536209(CHEMBL4539949)
Affinity DataIC50:  4nMAssay Description:Inhibition of human Gst-tagged JAK1 (850 to 1154 residues) expressed in baculovirus using biotin-synthetic peptide as substrate after 40 mins by HTRF...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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