BDBM296814 US10112942, Example 549::US10137124, Example 549::US10172851, Example 549::US10555944, Example 554::US10953005, Example 554

SMILES COc1ncc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OCCN3CCOCC3)cn3ncc(C#N)c23)cc1Cl

InChI Key InChIKey=QASIGBCVVWKQIP-UHFFFAOYSA-N

Data  21 IC50

  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 21 hits for monomerid = 296814   

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 144nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
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LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 727nMAssay Description:RET G810R: The potency of a compound inhibiting G810R mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
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LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 207nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Array Biopharma

US Patent
LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 19nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 535nMAssay Description:RET G810R: The potency of a compound inhibiting G810R mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 144nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Array Biopharma

US Patent
LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 10nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2021
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 727nMAssay Description:The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 207nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 19nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 535nMAssay Description:The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Array Biopharma

US Patent
LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 10nMpH: 7.4Assay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 10nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 535nMAssay Description:The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 144nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 10nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 535nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 144nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Array Biopharma

US Patent
LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 10nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 535nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2019
Entry Details
Go to US Patent

LigandPNGBDBM296814(US10112942, Example 549 | US10137124, Example 549 ...)
Affinity DataIC50: 144nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2019
Entry Details
Go to US Patent