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TargetCREB-binding protein(Human)
Pfizer

LigandPNGBDBM188516(BDOIA383)
Affinity DataKd:  120nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
LigandPNGBDBM188516(BDOIA383)
Affinity DataKd:  780nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Pfizer

LigandPNGBDBM188517(PF-CBP1)
Affinity DataKd:  190nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
LigandPNGBDBM188517(PF-CBP1)
Affinity DataKd: >2.00E+4nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
TargetCREB-binding protein(Human)
Pfizer

LigandPNGBDBM188519(SGC-CBP30)
Affinity DataKd:  21nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
LigandPNGBDBM188519(SGC-CBP30)
Affinity DataKd:  850nMAssay Description:Experiments were performed using recombinant CBP and BRD4 bromodomainsusing the procedure reported recently (Hett et al., 2015).More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/29/2016
Entry Details Article
PubMed
TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394655(US10308615, Example 12 | preparation of {2-[(pyrid...)
Affinity DataIC50: 0.5nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394660(US10308615, Example 17 | preparation of [3-(methyl...)
Affinity DataIC50: 0.800nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189904(US9670201, 29 (S)-3-cyano-N-(1-methyl-3-(1-(tetrah...)
Affinity DataIC50: 0.900nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
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TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411418(US10385036, Example 34 | N-(3-((3R,4R)-1-((R)-2-cy...)
Affinity DataIC50: 0.900nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
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TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189904(US9670201, 29 (S)-3-cyano-N-(1-methyl-3-(1-(tetrah...)
Affinity DataIC50: 0.900nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
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TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411412(US10385036, Example 28 | (R)-2-fluoro-N-(1-methyl-...)
Affinity DataIC50: 1nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
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TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411419(US10385036, Example 35 | N-(3-((3R,4R)-1-((R)-2-cy...)
Affinity DataIC50: 1nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
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LigandPNGBDBM50152828(Apatinib | YN-968D1)
Affinity DataIC50: 1nMAssay Description:Inhibition of VEGF2 receptor (unknown origin) by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2017
Entry Details Article
PubMed
TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411417(US10385036, Example 33 | N-(3-((3R,4R)-1-((R)-2-cy...)
Affinity DataIC50: 1.10nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM190325(US9670201, 81 3-cyano-N-(3-((3R,4R)-1-(cyclopentan...)
Affinity DataIC50: 1.20nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM395062(US10308615, Example 73 | (2-{[(6- methylpyridin-3-...)
Affinity DataIC50: 1.20nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM190325(US9670201, 81 3-cyano-N-(3-((3R,4R)-1-(cyclopentan...)
Affinity DataIC50: 1.20nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
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TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411410(US10385036, Example 26 | (R)-1,3,5-trimethyl-N-(1-...)
Affinity DataIC50: 1.30nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
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TargetDipeptidyl peptidase 4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50335784(2-[6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human recombinant DPP4 using Gly-Pro-7-amido-4-methyl-coumarin as substrate incubated for 15 mins by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189884(US9670201, 11 4-chloro-3-cyano-N-(3-(1-isobutyrylp...)
Affinity DataIC50: 1.5nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189884(US9670201, 11 4-chloro-3-cyano-N-(3-(1-isobutyrylp...)
Affinity DataIC50: 1.5nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394659(US10308615, Example 16 | preparation of (2-{[1-(py...)
Affinity DataIC50: 1.70nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM395062(US10308615, Example 73 | (2-{[(6- methylpyridin-3-...)
Affinity DataIC50: 1.70nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411411(US10385036, Example 27 | (R)-2-ethoxy-N-(1-methyl-...)
Affinity DataIC50: 1.70nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394660(US10308615, Example 17 | preparation of [3-(methyl...)
Affinity DataIC50: 1.80nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394655(US10308615, Example 12 | preparation of {2-[(pyrid...)
Affinity DataIC50: 1.90nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394656(US10308615, Example 13 | [3-(methylsulfonyl)phenyl...)
Affinity DataIC50: 2nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM368656(3-cyano-N-(3-((1R,5S,8r)-3-isobutyryl-3- azabicycl...)
Affinity DataIC50: 2.10nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394645(US10308615, Example 2 | 3-[(2-{[1-(pyridin-3-yl)cy...)
Affinity DataIC50: 2.10nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411409(US10385036, Example 25 | (R)-4-methyl-N-(1-methyl-...)
Affinity DataIC50: 2.10nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM368656(3-cyano-N-(3-((1R,5S,8r)-3-isobutyryl-3- azabicycl...)
Affinity DataIC50: 2.10nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411415(US10385036, Example 31 | (R)-N-(3-(1-(2-(bicyclo[1...)
Affinity DataIC50: 2.40nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411416(US10385036, Example 32 | N-(3-((3R,4R)-1-((R)-2-cy...)
Affinity DataIC50: 2.5nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394659(US10308615, Example 16 | preparation of (2-{[1-(py...)
Affinity DataIC50: 2.60nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189895(US9670201, 22 (S)-3-cyano-N-(1-methyl-4-(trifluoro...)
Affinity DataIC50: 2.70nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM190346(US9670201, 95 3-cyano-N-(3-((2S,4R)-1-isobutyryl-2...)
Affinity DataIC50: 2.70nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189895(US9670201, 22 (S)-3-cyano-N-(1-methyl-4-(trifluoro...)
Affinity DataIC50: 2.70nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM190346(US9670201, 95 3-cyano-N-(3-((2S,4R)-1-isobutyryl-2...)
Affinity DataIC50: 2.70nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189905(US9670201, 30 (R)-3-cyano-4-methoxy-N-(1-methyl-4-...)
Affinity DataIC50: 2.80nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189905(US9670201, 30 (R)-3-cyano-4-methoxy-N-(1-methyl-4-...)
Affinity DataIC50: 2.80nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394655(US10308615, Example 12 | preparation of {2-[(pyrid...)
Affinity DataIC50: 2.90nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
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TargetTyrosine-protein kinase BTK(Human)
Seattle Genetics

Curated by ChEMBL
LigandPNGBDBM50175583(ACP-196 | Acalabrutinib | US9758524, Example 6 | U...)
Affinity DataIC50: 3nMAssay Description:Inhibition of BTK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM411400(US10385036, Example 16 | (S)-N-(3-(1-(2,3-dimethyl...)
Affinity DataIC50: 3.10nMAssay Description:In general, the assay is based on the interaction between N-terminally Six-Histidine-tagged-RORC2 ligand binding domain (6-His-RORC2 LBD), expressed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189874(US9670201, 3 3-cyano-N-(3-(1-(cyclopentanecarbonyl...)
Affinity DataIC50: 3.20nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189874(US9670201, 3 3-cyano-N-(3-(1-(cyclopentanecarbonyl...)
Affinity DataIC50: 3.20nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM50466890(CHEMBL4290728)
Affinity DataIC50: 3.30nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM394648(US10308615, Example 5 | 3-[(2-{[1-(pyrazin-2-yl)cy...)
Affinity DataIC50: 3.40nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetPantetheinase(Human)
Pfizer

US Patent
LigandPNGBDBM395070(US10308615, Example 81 | [4-fluoro-3- (trifluorome...)
Affinity DataIC50: 3.40nMAssay Description:The vanin-1 protein was prepared in-house from a construct expressing the extracellular domain of human vanin-1 (GenBank ID NM_004666) preceded N-ter...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent

TargetNuclear receptor ROR-gamma(Human)
Pfizer

US Patent
LigandPNGBDBM189882(US9670201, 10 3-chloro-N-(3-(1-isobutyrylpiperidin...)
Affinity DataIC50: 3.5nMAssay Description:The activity of compound of the invention can be determined by a co-activator recruitment by TR-FRET (time-resolved fluorescence resonance energy tra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2019
Entry Details
Go to US Patent

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