BDBM50382959 CEP-32496::CHEMBL2029988::US9730937, Example 261

SMILES COc1cc2ncnc(Oc3cccc(NC(=O)Nc4cc(on4)C(C)(C)C(F)(F)F)c3)c2cc1OC

InChI Key InChIKey=DKNUPRMJNUQNHR-UHFFFAOYSA-N

Data  20 IC50  42 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 62 hits for monomerid = 50382959   

TargetVascular endothelial growth factor receptor 1(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  14nMAssay Description:Binding affinity to FLT-1 (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  8nMAssay Description:Inhibition of VEGFR2 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2C19(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 3.40E+3nMAssay Description:Inhibition of human CYP2C19More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: <250nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSerine/threonine-protein kinase B-raf(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: <250nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: <250nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: <250nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSerine/threonine-protein kinase B-raf(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  375nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: <250nMAssay Description:Competition binding assays used herein were developed, validated and performed as described in Fabian et al., Nature Biotechnology 2005, 23, 329-336....More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 2nMAssay Description:Inhibition of human RET kinase using IGF1Rtide as substrate incubated for 40 mins and measured by ADP-Glo assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  1.5nMAssay Description:Binding affinity to RET (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  36nMAssay Description:Binding affinity to BRAF (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  14nMAssay Description:Binding affinity to BRAF V600E (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  39nMAssay Description:Binding affinity to CRAF (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetTyrosine-protein kinase ABL1(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  2.80nMAssay Description:Binding affinity to ABL (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  7.90nMAssay Description:Binding affinity to VEGFR2 (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  2nMAssay Description:Inhibition of Ret in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMast/stem cell growth factor receptor Kit(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  2.40nMAssay Description:Binding affinity to C-KIT (unknown origin) assessed as dissociation constant measured by ambit kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 7nMAssay Description:Inhibition of RET (unknown origin) by kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 146nMAssay Description:Inhibition of CRAF (unknown origin) by kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetTyrosine-protein kinase ABL1(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 6nMAssay Description:Inhibition of ABL (unknown origin) by kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 43nMAssay Description:Inhibition of VEGFR2 (unknown origin) by kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetCoiled-coil domain-containing protein 6(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of CCDC6-RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 0.410nMAssay Description:Inhibition of NCOA4-RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 4.30nMAssay Description:Inhibition of RET M918T (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 319nMAssay Description:Inhibition of RET V804L (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 31nMAssay Description:Inhibition of wildtype RET (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 168nMAssay Description:Inhibition of recombinant RET V804L (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
University of Gothenburg

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant RET M918T (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 17nMAssay Description:Inhibition of recombinant VEGFR2 (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetCoiled-coil domain-containing protein 6(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 7nMAssay Description:Inhibition of recombinant CCDC6-RET (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  36nMAssay Description:Inhibition of wild type BRAF in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEphrin type-A receptor 2 [596-900](Human)
Technical University of Munich

LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 28nMAssay Description:Refer to Reaction Biology Corps.More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAurora kinase B(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of Aurora B in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 3A4(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human CYP3A4More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2D6(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human CYP2D6More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2C9(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human CYP2C9More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 1A2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human CYP1A2More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of ERK2 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMitogen-activated protein kinase 3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of ERK1 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEphrin type-A receptor 2(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  14nMAssay Description:Inhibition of EPHA2 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEpidermal growth factor receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  22nMAssay Description:Inhibition of EGFR in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  9nMAssay Description:Inhibition of CSF1R in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAurora kinase A(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of Aurora A in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of ALK in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase ABL1(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  3nMAssay Description:Inhibition of Abl1 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Ambit Biosciences

US Patent
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  39nMAssay Description:Inhibition of CRAF in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEphrin type-A receptor 2 [596-900](Human)
Technical University of Munich

LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd:  99nMAssay Description:Kinobeads competition assays were performed in 96-well format as previously described using mixed protein lysates of four cancer cell lines (K-562, M...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetIGF-like family receptor 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of IGFR1 in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50382959(CEP-32496 | CHEMBL2029988 | US9730937, Example 261)
Affinity DataKd: >1.00E+4nMAssay Description:Inhibition of INSR in human HEK293 cells after 1 hr by competition binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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