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TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394530(US10308614, Example 131 | (R)-1-(4-(3-amino-6-(2-)
Affinity DataKd:  16nMAssay Description:Binding affinity to human SMARCA2 (S1337 to Q1486 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
Merck Frosst Centre For Therapeutic Research

Curated by ChEMBL
LigandPNGBDBM50333850((R)-2-(7-(4-fluoro-N-(4-fluorobenzyl)phenylsulfona...)
Affinity DataEC50: >3.00E+4nMAssay Description:Induction of pregnane X receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2011
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613459(CHEMBL5287013)
Affinity DataEC50:  250nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613469(CHEMBL5279452)
Affinity DataEC50:  1.10E+3nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
Merck Frosst Centre For Therapeutic Research

Curated by ChEMBL
LigandPNGBDBM50333844((R)-2-(4-fluoro-7-(4-fluoro-N-methylphenylsulfonam...)
Affinity DataEC50: >3.00E+4nMAssay Description:Induction of pregnane X receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2011
Entry Details Article
PubMed
TargetTranscription activator BRG1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598934(CHEMBL5183240)
Affinity DataKd:  510nMAssay Description:Binding affinity to human SMARCA4 (A1448 to S1575 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394583(US10308614, Example 186 | 2-(6-amino-5-phenylpyrid...)
Affinity DataKd:  1.10E+3nMAssay Description:Binding affinity to human MHHHHHHGSLVPRGS-tagged SMARAC2 isoform B L1412P/P1413V/S1414N mutant (S1377 to Q1486 residues) by isothermal titration calo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetProtein polybromo-1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598934(CHEMBL5183240)
Affinity DataKd:  580nMAssay Description:Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613461(CHEMBL5274793)
Affinity DataEC50:  170nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetProtein polybromo-1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394530(US10308614, Example 131 | (R)-1-(4-(3-amino-6-(2-)
Affinity DataKd:  18nMAssay Description:Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetProtein polybromo-1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598935(CHEMBL5194650)
Affinity DataKd:  5.70E+3nMAssay Description:Binding affinity to human PBRM1 bromodomain 2 (S178 to E291 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178170(CHEMBL3814881)
Affinity DataEC50: >1.00E+4nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
Merck Frosst Centre For Therapeutic Research

Curated by ChEMBL
LigandPNGBDBM50333868((R)-2-(3-fluoro-7-(4-fluoro-N-methylphenylsulfonam...)
Affinity DataEC50: >3.00E+4nMAssay Description:Induction of pregnane X receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2011
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613458(CHEMBL5266575)
Affinity DataEC50:  100nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613452(CHEMBL5269306)
Affinity DataEC50:  720nMAssay Description:Inhibition of BRD4 BD1 in human Raji cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613467(CHEMBL5276602)
Affinity DataEC50: >4.00E+3nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613471(CHEMBL5276365)
Affinity DataEC50:  440nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613463(CHEMBL5277826)
Affinity DataEC50:  140nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetTranscription activator BRG1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598935(CHEMBL5194650)
Affinity DataKd:  1.00E+4nMAssay Description:Binding affinity to human SMARCA4 (A1448 to S1575 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178164(CHEMBL3815023 | US10206931, Example 173)
Affinity DataEC50:  3.40E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613455(CHEMBL5288449)
Affinity DataEC50:  270nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394530(US10308614, Example 131 | (R)-1-(4-(3-amino-6-(2-)
Affinity DataEC50:  100nMAssay Description:Inhibition of SMARAC2 isoform B (unknown origin) expressed in U2OS cells co-expressed in NLS-ZsGreen incubated for 1 hrs by cellular target engagemen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613462(CHEMBL5280537)
Affinity DataEC50:  170nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetLysine-specific demethylase 5A(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM195608(CPI-455 | US20240139197, Compound 3)
Affinity DataEC50:  5.20E+3nMAssay Description:Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 levels preincubated for 4 days measured up to 24 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613465(CHEMBL5271336)
Affinity DataEC50:  33nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetProtein polybromo-1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598935(CHEMBL5194650)
Affinity DataKd:  2.70E+4nMAssay Description:Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetTranscription activator BRG1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394530(US10308614, Example 131 | (R)-1-(4-(3-amino-6-(2-)
Affinity DataKd:  47nMAssay Description:Binding affinity to His6/FLAG-tagged SMARCA4 (unknown origin) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178219(CHEMBL3814752)
Affinity DataKd:  30nMAssay Description:Binding affinity to human CBP at 17 uM by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178220(CHEMBL3814550 | US10206931, Example 57)
Affinity DataEC50:  3.00E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178163(CHEMBL3813846 | US10206931, Example 286)
Affinity DataEC50: >1.00E+4nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394583(US10308614, Example 186 | 2-(6-amino-5-phenylpyrid...)
Affinity DataKd:  71nMAssay Description:Binding affinity to human SMARCA2 (S1337 to Q1486 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178221(CHEMBL3814602)
Affinity DataEC50:  7.00E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178218(CHEMBL3814595)
Affinity DataEC50: >1.00E+4nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613466(CHEMBL5283924)
Affinity DataEC50:  30nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178219(CHEMBL3814752)
Affinity DataEC50:  300nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613468(CHEMBL5273382)
Affinity DataEC50:  2.60E+3nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178162(CHEMBL3814197)
Affinity DataEC50:  8.10E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50598935(CHEMBL5194650)
Affinity DataKd:  4.40E+3nMAssay Description:Binding affinity to human SMARCA2 (S1337 to Q1486 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetProtein polybromo-1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM50158688(CHEMBL3752911)
Affinity DataKd:  5.80E+3nMAssay Description:Binding affinity to human PBRM1 bromodomain 2 (S178 to E291 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178175(CHEMBL3813915)
Affinity DataEC50: >1.00E+4nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613470(CHEMBL5273860)
Affinity DataEC50:  2.90E+3nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394583(US10308614, Example 186 | 2-(6-amino-5-phenylpyrid...)
Affinity DataEC50:  300nMAssay Description:Inhibition of SMARAC2 isoform B (unknown origin) expressed in U2OS cells co-expressed in NLS-ZsGreen incubated for 1 hrs by cellular target engagemen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetProbable global transcription activator SNF2L2(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394583(US10308614, Example 186 | 2-(6-amino-5-phenylpyrid...)
Affinity DataKd:  61nMAssay Description:Binding affinity to human MHHHHHHGSLVPRGS-tagged SMARAC2 isoform B (S1377 to Q1486 residues) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetLysine-specific demethylase 5A(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM195608(CPI-455 | US20240139197, Compound 3)
Affinity DataEC50:  5.20E+3nMAssay Description:Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 levels preincubated for 4 days measured up to 24 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613454(CHEMBL5289896)
Affinity DataEC50:  210nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178161(CHEMBL3813929)
Affinity DataEC50:  1.90E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50178168(CHEMBL3814246 | US10206931, Example 176)
Affinity DataEC50:  5.00E+3nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter ge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613460(CHEMBL5290918)
Affinity DataEC50:  220nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetBromodomain-containing protein 4(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50613457(CHEMBL5282917)
Affinity DataEC50:  4.00E+3nMAssay Description:Inhibition of BRD4 BD1 in human MV4-11 cells assessed as reduction of MYC RNA expression after 4 hrs by PCR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetTranscription activator BRG1(Human)
Constellation, A Morphosys

Curated by ChEMBL
LigandPNGBDBM394583(US10308614, Example 186 | 2-(6-amino-5-phenylpyrid...)
Affinity DataKd:  86nMAssay Description:Binding affinity to human SMARCA4 (A1448 to S1575 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
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