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Compile Data Set for Download or QSAR

Found 9123 hits of ic50 for UniProtKB: P48736   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326285
PNG
(US9637488, 68)
Show SMILES Nc1nc(N)c(C#N)c(n1)N1CCCC1c1cc2cccc(Cl)c2nc1-c1ccccc1
Show InChI InChI=1S/C24H20ClN7/c25-18-9-4-8-15-12-16(20(29-21(15)18)14-6-2-1-3-7-14)19-10-5-11-32(19)23-17(13-26)22(27)30-24(28)31-23/h1-4,6-9,12,19H,5,10-11H2,(H4,27,28,30,31)
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n/an/a<0.0500n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326267
PNG
(US9637488, 27)
Show SMILES Nc1nc(N)c(C#N)c(n1)N1CCCC1c1cc2ccc(F)cc2nc1-c1ccccc1
Show InChI InChI=1S/C24H20FN7/c25-16-9-8-15-11-17(21(29-19(15)12-16)14-5-2-1-3-6-14)20-7-4-10-32(20)23-18(13-26)22(27)30-24(28)31-23/h1-3,5-6,8-9,11-12,20H,4,7,10H2,(H4,27,28,30,31)
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n/an/a<0.0500n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326282
PNG
(US9637488, 65)
Show SMILES Cc1cccc2cc([C@H]3CCCN3c3ncnc(N)c3C#N)c(nc12)N1CCOCC1
Show InChI InChI=1S/C23H25N7O/c1-15-4-2-5-16-12-17(23(28-20(15)16)29-8-10-31-11-9-29)19-6-3-7-30(19)22-18(13-24)21(25)26-14-27-22/h2,4-5,12,14,19H,3,6-11H2,1H3,(H2,25,26,27)/t19-/m1/s1
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n/an/a<0.0500n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326284
PNG
(US9637488, 67)
Show SMILES Nc1ncnc(N2CCCC2c2cc3cccc(Cl)c3nc2-c2ccccc2)c1C#N
Show InChI InChI=1S/C24H19ClN6/c25-19-9-4-8-16-12-17(21(30-22(16)19)15-6-2-1-3-7-15)20-10-5-11-31(20)24-18(13-26)23(27)28-14-29-24/h1-4,6-9,12,14,20H,5,10-11H2,(H2,27,28,29)
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TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326278
PNG
(US9637488, 54)
Show SMILES Nc1nc(N)c(C#N)c(n1)N1CCC[C@H]1c1cc2cccc(Cl)c2nc1-c1ccccc1
Show InChI InChI=1S/C24H20ClN7/c25-18-9-4-8-15-12-16(20(29-21(15)18)14-6-2-1-3-7-14)19-10-5-11-32(19)23-17(13-26)22(27)30-24(28)31-23/h1-4,6-9,12,19H,5,10-11H2,(H4,27,28,30,31)/t19-/m0/s1
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TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326286
PNG
(US9637488, 69)
Show SMILES Nc1ncnc(N2CCC[C@@H]2c2cc3cccc(Cl)c3nc2N2CCOCC2)c1C#N
Show InChI InChI=1S/C22H22ClN7O/c23-17-4-1-3-14-11-15(22(28-19(14)17)29-7-9-31-10-8-29)18-5-2-6-30(18)21-16(12-24)20(25)26-13-27-21/h1,3-4,11,13,18H,2,5-10H2,(H2,25,26,27)/t18-/m1/s1
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n/an/a<0.0500n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326259
PNG
(US9637488, 18)
Show SMILES Nc1ncnc(N2CCCC2c2cc3ccc(F)cc3nc2N2CCCCC2)c1C#N
Show InChI InChI=1S/C23H24FN7/c24-16-7-6-15-11-17(23(29-19(15)12-16)30-8-2-1-3-9-30)20-5-4-10-31(20)22-18(13-25)21(26)27-14-28-22/h6-7,11-12,14,20H,1-5,8-10H2,(H2,26,27,28)
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n/an/a 0.100n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50192880
PNG
(CHEMBL3984425 | US10329299, Compound 21 | US106752...)
Show SMILES C[C@H](NC(=O)c1c(N)nn2cccnc12)c1cc2cccc(C#Cc3cnn(C)c3)c2c(=O)n1-c1ccccc1 |r|
Show InChI InChI=1S/C30H24N8O2/c1-19(34-29(39)26-27(31)35-37-15-7-14-32-28(26)37)24-16-22-9-6-8-21(13-12-20-17-33-36(2)18-20)25(22)30(40)38(24)23-10-4-3-5-11-23/h3-11,14-19H,1-2H3,(H2,31,35)(H,34,39)/t19-/m0/s1
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n/an/a 0.290n/an/an/an/an/an/a



China Pharmaceutical University

Curated by ChEMBL


Assay Description
Inhibition of PI3Kgamma (unknown origin)


Eur J Med Chem 163: 413-427 (2019)


Article DOI: 10.1016/j.ejmech.2018.11.072
BindingDB Entry DOI: 10.7270/Q2736V7K
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50450680
PNG
(CHEMBL4168702)
Show SMILES COc1cc(ccc1O)-c1c[nH]c2ncnc(N[C@@H](C)c3nn4ccc(C)c4c(=O)n3-c3ccccc3)c12 |r|
Show InChI InChI=1S/C28H25N7O3/c1-16-11-12-34-24(16)28(37)35(19-7-5-4-6-8-19)27(33-34)17(2)32-26-23-20(14-29-25(23)30-15-31-26)18-9-10-21(36)22(13-18)38-3/h4-15,17,36H,1-3H3,(H2,29,30,31,32)/t17-/m0/s1
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n/an/a 0.300n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate a...


J Med Chem 61: 9551-9567 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00873
BindingDB Entry DOI: 10.7270/Q2GB26MQ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474011
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-({[1-(fluorome...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)NCC1(CCF)CC1)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C25H31FN4O4S2/c1-14-22(35-24(28-14)29-16(3)31)18-10-19-12-30(15(2)17-4-5-17)23(32)21(19)20(11-18)36(33,34)27-13-25(6-7-25)8-9-26/h10-11,15,17,27H,4-9,12-13H2,1-3H3,(H,28,29,31)/t15-/m0/s1
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n/an/a 0.398n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474007
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-(ethylsulfamoy...)
Show SMILES CCNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C21H26N4O4S2/c1-5-22-31(28,29)17-9-15(19-11(2)23-21(30-19)24-13(4)26)8-16-10-25(20(27)18(16)17)12(3)14-6-7-14/h8-9,12,14,22H,5-7,10H2,1-4H3,(H,23,24,26)/t12-/m0/s1
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n/an/a 0.398n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50145416
PNG
(GSK2126458 | Omipalisib)
Show SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccnnc3)c2c1
Show InChI InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
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n/an/a 0.440n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant human full-length His-tagged PI3Kgamma expressed in baculovirus expression system using PIP2 as substrate measured after 1 ...


Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113249
BindingDB Entry DOI: 10.7270/Q2PC3641
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50457159
PNG
(CHEMBL4217725)
Show SMILES Clc1ncc(cc1NS(=O)(=O)c1ccccc1)-c1cnc2[nH]cc(-c3ccncc3)c2c1
Show InChI InChI=1S/C23H16ClN5O2S/c24-22-21(29-32(30,31)18-4-2-1-3-5-18)11-17(12-26-22)16-10-19-20(14-28-23(19)27-13-16)15-6-8-25-9-7-15/h1-14,29H,(H,27,28)
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n/an/a 0.5n/an/an/an/an/an/a



Fudan University

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 h...


ACS Med Chem Lett 8: 875-880 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00222
BindingDB Entry DOI: 10.7270/Q2CR5WZT
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326262
PNG
(US9637488, 22 | US9637488, 24)
Show SMILES Fc1ccc2cc(C3CCCN3c3ncnc4[nH]cnc34)c(nc2c1)-c1ccccc1F
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n/an/a 0.5n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474028
PNG
(N-(5-{7-[(3-Cyanophenyl)sulfamoyl]-2-[(1S)-1-cyclo...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)Nc1cccc(c1)C#N)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C26H25N5O4S2/c1-14-24(36-26(28-14)29-16(3)32)19-10-20-13-31(15(2)18-7-8-18)25(33)23(20)22(11-19)37(34,35)30-21-6-4-5-17(9-21)12-27/h4-6,9-11,15,18,30H,7-8,13H2,1-3H3,(H,28,29,32)/t15-/m0/s1
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n/an/a 0.501n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50546014
PNG
(CHEMBL4780201)
Show SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2ncnc(Nc3cnn(CCO)c3)c2c1
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n/an/a 0.580n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PI3Kgamma (unknown origin) using lipid as substrate incubated for 15 mins followed by substrate addition and measured after 60 mins ADP...


Citation and Details

Article DOI: 10.1016/j.bmc.2019.04.024
BindingDB Entry DOI: 10.7270/Q2T1577B
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM236931
PNG
(US9388189, 27)
Show SMILES C[C@H](Nc1ncnc2[nH]cc(-c3cc(O)cc(F)c3)c12)c1nn2ccc(C)c2c(=O)n1-c1ccccc1
Show InChI InChI=1S/C27H22FN7O2/c1-15-8-9-34-23(15)27(37)35(19-6-4-3-5-7-19)26(33-34)16(2)32-25-22-21(13-29-24(22)30-14-31-25)17-10-18(28)12-20(36)11-17/h3-14,16,36H,1-2H3,(H2,29,30,31,32)/t16-/m0/s1
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n/an/a 0.600n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate a...


J Med Chem 61: 9551-9567 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00873
BindingDB Entry DOI: 10.7270/Q2GB26MQ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50145416
PNG
(GSK2126458 | Omipalisib)
Show SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccnnc3)c2c1
Show InChI InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
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n/an/a 0.600n/an/an/an/an/an/a



Second Military Medical University

Curated by ChEMBL


Assay Description
Inhibition of PI3K-gamma (unknown origin) after 40 mins by ADP-Glo luminescent kinase assay


Bioorg Med Chem 24: 957-66 (2016)


Article DOI: 10.1016/j.bmc.2016.01.008
BindingDB Entry DOI: 10.7270/Q2DF6T2X
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50433545
PNG
(CHEMBL2381271)
Show SMILES CC(C)n1ncnc1-c1nc-2c(CCOc3cc(ccc-23)-c2cn(C)cn2)s1
Show InChI InChI=1S/C20H20N6OS/c1-12(2)26-19(21-10-23-26)20-24-18-14-5-4-13(15-9-25(3)11-22-15)8-16(14)27-7-6-17(18)28-20/h4-5,8-12H,6-7H2,1-3H3
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n/an/a 0.600n/an/an/an/an/an/a



Genentech, Inc.

Curated by ChEMBL


Assay Description
Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...


Bioorg Med Chem Lett 23: 2606-13 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.102
BindingDB Entry DOI: 10.7270/Q2W95BKF
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50145416
PNG
(GSK2126458 | Omipalisib)
Show SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccnnc3)c2c1
Show InChI InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
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n/an/a 0.610n/an/an/an/an/an/a



Second Military Medical University

Curated by ChEMBL


Assay Description
Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assay


Eur J Med Chem 122: 684-701 (2016)


Article DOI: 10.1016/j.ejmech.2016.06.030
BindingDB Entry DOI: 10.7270/Q2VD71FD
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274660
PNG
(CHEMBL4128537 | US10858355, Example 12)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(N)(=O)=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C19H22N4O4S2/c1-9-17(28-19(21-9)22-11(3)24)13-6-14-8-23(10(2)12-4-5-12)18(25)16(14)15(7-13)29(20,26)27/h6-7,10,12H,4-5,8H2,1-3H3,(H2,20,26,27)(H,21,22,24)/t10-/m0/s1
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n/an/a 0.631n/an/an/an/an/an/a



Pharmaron-Beijing Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...


J Med Chem 61: 5435-5441 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00447
BindingDB Entry DOI: 10.7270/Q27M0BFZ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274640
PNG
(CHEMBL4126445)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(C)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H23N3O2S/c1-10-7-15(18-11(2)21-20(26-18)22-13(4)24)8-16-9-23(19(25)17(10)16)12(3)14-5-6-14/h7-8,12,14H,5-6,9H2,1-4H3,(H,21,22,24)/t12-/m0/s1
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n/an/a 0.631n/an/an/an/an/an/a



Pharmaron-Beijing Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...


J Med Chem 61: 5435-5441 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00447
BindingDB Entry DOI: 10.7270/Q27M0BFZ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274648
PNG
(CHEMBL4127396 | US10858355, Example 22)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(NS(C)(=O)=O)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(21-10)22-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)23-30(4,27)28/h7-8,11,13,23H,5-6,9H2,1-4H3,(H,21,22,25)/t11-/m0/s1
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Pharmaron-Beijing Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...


J Med Chem 61: 5435-5441 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00447
BindingDB Entry DOI: 10.7270/Q27M0BFZ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50579671
PNG
(CHEMBL5090959)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(Nc2cccc(n2)-c2ocnc2CO)nc1C |r|
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TBA

Assay Description
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00434
BindingDB Entry DOI: 10.7270/Q24Q7ZVJ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274648
PNG
(CHEMBL4127396 | US10858355, Example 22)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(NS(C)(=O)=O)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(21-10)22-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)23-30(4,27)28/h7-8,11,13,23H,5-6,9H2,1-4H3,(H,21,22,25)/t11-/m0/s1
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n/an/a 0.631n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274638
PNG
(CHEMBL4126156 | US10858355, Example 4)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H23N3O4S2/c1-10-18(28-20(21-10)22-12(3)24)14-7-15-9-23(11(2)13-5-6-13)19(25)17(15)16(8-14)29(4,26)27/h7-8,11,13H,5-6,9H2,1-4H3,(H,21,22,24)/t11-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474012
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-1-oxo-7-[(2,2,2-...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)NCC(F)(F)F)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C21H23F3N4O4S2/c1-10-18(33-20(26-10)27-12(3)29)14-6-15-8-28(11(2)13-4-5-13)19(30)17(15)16(7-14)34(31,32)25-9-21(22,23)24/h6-7,11,13,25H,4-5,8-9H2,1-3H3,(H,26,27,29)/t11-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474008
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-(oxetan-3-ylsu...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)NC1COC1)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C22H26N4O5S2/c1-11-20(32-22(23-11)24-13(3)27)15-6-16-8-26(12(2)14-4-5-14)21(28)19(16)18(7-15)33(29,30)25-17-9-31-10-17/h6-7,12,14,17,25H,4-5,8-10H2,1-3H3,(H,23,24,27)/t12-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474015
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-[(cyclopropyls...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(NS(=O)(=O)C3CC3)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C22H26N4O4S2/c1-11-20(31-22(23-11)24-13(3)27)15-8-16-10-26(12(2)14-4-5-14)21(28)19(16)18(9-15)25-32(29,30)17-6-7-17/h8-9,12,14,17,25H,4-7,10H2,1-3H3,(H,23,24,27)/t12-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50204093
PNG
(BAY 80-6946 | BAY-80-6946 | Copanlisib)
Show SMILES COc1c(OCCCN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cnc(N)nc3)=Nc12 |c:35,t:18|
Show InChI InChI=1S/C23H28N8O4/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15/h3-4,13-14H,2,5-12H2,1H3,(H2,24,26,27)(H,28,29,32)
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n/an/a 0.700n/an/an/an/an/an/a



Ain Shams University

Curated by ChEMBL


Assay Description
Inhibition of PI3Kgamma (unknown origin)


Eur J Med Chem 183: (2019)


Article DOI: 10.1016/j.ejmech.2019.111718
BindingDB Entry DOI: 10.7270/Q23J3HCB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM326261
PNG
(US9637488, 21)
Show SMILES Fc1ccc2cc(C3CCCN3c3ncnc4[nH]cnc34)c(nc2c1)-c1ccccc1
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n/an/a 0.700n/an/an/an/an/an/a



TBA

US Patent


Assay Description
Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...


US Patent US9637488 (2017)


BindingDB Entry DOI: 10.7270/Q2D220Q6
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50457173
PNG
(CHEMBL4213317)
Show SMILES Fc1ccccc1S(=O)(=O)Nc1cc(cnc1Cl)-c1cnc2[nH]cc(-c3ccncc3)c2c1
Show InChI InChI=1S/C23H15ClFN5O2S/c24-22-20(30-33(31,32)21-4-2-1-3-19(21)25)10-16(11-27-22)15-9-17-18(13-29-23(17)28-12-15)14-5-7-26-8-6-14/h1-13,30H,(H,28,29)
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n/an/a 0.700n/an/an/an/an/an/a



Fudan University

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 h...


ACS Med Chem Lett 8: 875-880 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00222
BindingDB Entry DOI: 10.7270/Q2CR5WZT
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50457170
PNG
(CHEMBL4208385)
Show SMILES Fc1ccc(cc1)S(=O)(=O)Nc1cc(cnc1Cl)-c1cnc2[nH]cc(-c3ccncc3)c2c1
Show InChI InChI=1S/C23H15ClFN5O2S/c24-22-21(30-33(31,32)18-3-1-17(25)2-4-18)10-16(11-27-22)15-9-19-20(13-29-23(19)28-12-15)14-5-7-26-8-6-14/h1-13,30H,(H,28,29)
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Fudan University

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 h...


ACS Med Chem Lett 8: 875-880 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00222
BindingDB Entry DOI: 10.7270/Q2CR5WZT
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50450695
PNG
(CHEMBL4176898)
Show SMILES C[C@H](Nc1ncnc2[nH]cc(-c3ccc(O)cc3)c12)c1nn2ccc(C)c2c(=O)n1-c1ccccc1 |r|
Show InChI InChI=1S/C27H23N7O2/c1-16-12-13-33-23(16)27(36)34(19-6-4-3-5-7-19)26(32-33)17(2)31-25-22-21(14-28-24(22)29-15-30-25)18-8-10-20(35)11-9-18/h3-15,17,35H,1-2H3,(H2,28,29,30,31)/t17-/m0/s1
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TBA

Curated by ChEMBL


Assay Description
Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate a...


J Med Chem 61: 9551-9567 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00873
BindingDB Entry DOI: 10.7270/Q2GB26MQ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50433559
PNG
(CHEMBL2381269)
Show SMILES CC(C)n1ncnc1-c1nc-2c(CCOc3cc(ccc-23)-c2cn[nH]c2)s1
Show InChI InChI=1S/C19H18N6OS/c1-11(2)25-18(20-10-23-25)19-24-17-14-4-3-12(13-8-21-22-9-13)7-15(14)26-6-5-16(17)27-19/h3-4,7-11H,5-6H2,1-2H3,(H,21,22)
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Genentech, Inc.

Curated by ChEMBL


Assay Description
Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presen...


Bioorg Med Chem Lett 23: 2606-13 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.102
BindingDB Entry DOI: 10.7270/Q2W95BKF
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50450675
PNG
(CHEMBL4166977)
Show SMILES C[C@H](Nc1ncnc2[nH]cc(-c3cc(O)cc(NS(C)(=O)=O)c3)c12)c1nn2ccc(C)c2c(=O)n1-c1ccccc1 |r|
Show InChI InChI=1S/C28H26N8O4S/c1-16-9-10-35-24(16)28(38)36(20-7-5-4-6-8-20)27(33-35)17(2)32-26-23-22(14-29-25(23)30-15-31-26)18-11-19(13-21(37)12-18)34-41(3,39)40/h4-15,17,34,37H,1-3H3,(H2,29,30,31,32)/t17-/m0/s1
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n/an/a 0.700n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate a...


J Med Chem 61: 9551-9567 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00873
BindingDB Entry DOI: 10.7270/Q2GB26MQ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50606726
PNG
(CHEMBL5220911)
Show SMILES CC(=O)N1CCN(CC1)c1cnc2ccc(cc2n1)-c1cnc(Cl)c(NS(=O)(=O)c2ccc(F)cc2)c1
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n/an/a 0.710n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2022.114498
BindingDB Entry DOI: 10.7270/Q2ZG6XB2
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50202547
PNG
(CHEMBL3968925)
Show SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccc(Cn4cncn4)cc3)c2c1
Show InChI InChI=1S/C30H22F2N6O3S/c1-41-30-28(37-42(39,40)29-9-7-23(31)14-26(29)32)13-22(15-35-30)21-6-8-27-25(12-21)24(10-11-34-27)20-4-2-19(3-5-20)16-38-18-33-17-36-38/h2-15,17-18,37H,16H2,1H3
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n/an/a 0.740n/an/an/an/an/an/a



Second Military Medical University

Curated by ChEMBL


Assay Description
Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assay


Eur J Med Chem 122: 684-701 (2016)


Article DOI: 10.1016/j.ejmech.2016.06.030
BindingDB Entry DOI: 10.7270/Q2VD71FD
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474017
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-[(ethylsulfony...)
Show SMILES CCS(=O)(=O)Nc1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C21H26N4O4S2/c1-5-31(28,29)24-17-9-15(19-11(2)22-21(30-19)23-13(4)26)8-16-10-25(20(27)18(16)17)12(3)14-6-7-14/h8-9,12,14,24H,5-7,10H2,1-4H3,(H,22,23,26)/t12-/m0/s1
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n/an/a 0.794n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274638
PNG
(CHEMBL4126156 | US10858355, Example 4)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H23N3O4S2/c1-10-18(28-20(21-10)22-12(3)24)14-7-15-9-23(11(2)13-5-6-13)19(25)17(15)16(8-14)29(4,26)27/h7-8,11,13H,5-6,9H2,1-4H3,(H,21,22,24)/t11-/m0/s1
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n/an/a 0.794n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274648
PNG
(CHEMBL4127396 | US10858355, Example 22)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(NS(C)(=O)=O)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(21-10)22-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)23-30(4,27)28/h7-8,11,13,23H,5-6,9H2,1-4H3,(H,21,22,25)/t11-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274649
PNG
(CHEMBL4129600 | US10858355, Example 30)
Show SMILES CNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(22-10)23-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)30(27,28)21-4/h7-8,11,13,21H,5-6,9H2,1-4H3,(H,22,23,25)/t11-/m0/s1
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n/an/a 0.794n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474020
PNG
(US10858355, Example 28)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(NS(=O)(=O)CC3CC3)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C23H28N4O4S2/c1-12-21(32-23(24-12)25-14(3)28)17-8-18-10-27(13(2)16-6-7-16)22(29)20(18)19(9-17)26-33(30,31)11-15-4-5-15/h8-9,13,15-16,26H,4-7,10-11H2,1-3H3,(H,24,25,28)/t13-/m0/s1
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n/an/a 0.794n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM473999
PNG
(N-(5-{2-[(1S)-1-Cyclopropylethyl]-7-(dimethylsulfa...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)N(C)C)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C21H26N4O4S2/c1-11-19(30-21(22-11)23-13(3)26)15-8-16-10-25(12(2)14-6-7-14)20(27)18(16)17(9-15)31(28,29)24(4)5/h8-9,12,14H,6-7,10H2,1-5H3,(H,22,23,26)/t12-/m0/s1
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n/an/a 0.794n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
The activity of recombinant human PI3Kγ (aa144-1102)-6His was determined by measuring the ADP level after phosphorylation of DiC8-PIP2 using a c...


US Patent US10858355 (2020)


BindingDB Entry DOI: 10.7270/Q2BZ6945
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274649
PNG
(CHEMBL4129600 | US10858355, Example 30)
Show SMILES CNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(22-10)23-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)30(27,28)21-4/h7-8,11,13,21H,5-6,9H2,1-4H3,(H,22,23,25)/t11-/m0/s1
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TBA

Assay Description
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00434
BindingDB Entry DOI: 10.7270/Q24Q7ZVJ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274638
PNG
(CHEMBL4126156 | US10858355, Example 4)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H23N3O4S2/c1-10-18(28-20(21-10)22-12(3)24)14-7-15-9-23(11(2)13-5-6-13)19(25)17(15)16(8-14)29(4,26)27/h7-8,11,13H,5-6,9H2,1-4H3,(H,21,22,24)/t11-/m0/s1
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TBA

Assay Description
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00434
BindingDB Entry DOI: 10.7270/Q24Q7ZVJ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274649
PNG
(CHEMBL4129600 | US10858355, Example 30)
Show SMILES CNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C20H24N4O4S2/c1-10-18(29-20(22-10)23-12(3)25)14-7-15-9-24(11(2)13-5-6-13)19(26)17(15)16(8-14)30(27,28)21-4/h7-8,11,13,21H,5-6,9H2,1-4H3,(H,22,23,25)/t11-/m0/s1
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Pharmaron-Beijing Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...


J Med Chem 61: 5435-5441 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00447
BindingDB Entry DOI: 10.7270/Q27M0BFZ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM50274675
PNG
(CHEMBL4126601)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(Cl)c2C1=O)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C19H20ClN3O2S/c1-9-17(26-19(21-9)22-11(3)24)13-6-14-8-23(10(2)12-4-5-12)18(25)16(14)15(20)7-13/h6-7,10,12H,4-5,8H2,1-3H3,(H,21,22,24)/t10-/m0/s1
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Pharmaron-Beijing Co., Ltd

Curated by ChEMBL


Assay Description
Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substr...


J Med Chem 61: 5435-5441 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00447
BindingDB Entry DOI: 10.7270/Q27M0BFZ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM474028
PNG
(N-(5-{7-[(3-Cyanophenyl)sulfamoyl]-2-[(1S)-1-cyclo...)
Show SMILES C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)Nc1cccc(c1)C#N)-c1sc(NC(C)=O)nc1C |r|
Show InChI InChI=1S/C26H25N5O4S2/c1-14-24(36-26(28-14)29-16(3)32)19-10-20-13-31(15(2)18-7-8-18)25(33)23(20)22(11-19)37(34,35)30-21-6-4-5-17(9-21)12-27/h4-6,9-11,15,18,30H,7-8,13H2,1-3H3,(H,28,29,32)/t15-/m0/s1
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TBA

Assay Description
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00434
BindingDB Entry DOI: 10.7270/Q24Q7ZVJ
More data for this
Ligand-Target Pair
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform


(Homo sapiens (Human))
BDBM489240
PNG
(N-{6-[(5-{2-[(1S)-1-Cyclopropylethyl]-7-(methylsul...)
Show SMILES CNS(=O)(=O)c1cc(cc2CN([C@@H](C)C3CC3)C(=O)c12)-c1sc(Nc2cccc(n2)N(C)C(C)=O)nc1C |r|
Show InChI InChI=1S/C26H30N6O4S2/c1-14-24(37-26(28-14)30-21-7-6-8-22(29-21)31(5)16(3)33)18-11-19-13-32(15(2)17-9-10-17)25(34)23(19)20(12-18)38(35,36)27-4/h6-8,11-12,15,17,27H,9-10,13H2,1-5H3,(H,28,29,30)/t15-/m0/s1
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TBA

Assay Description
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by su...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00434
BindingDB Entry DOI: 10.7270/Q24Q7ZVJ
More data for this
Ligand-Target Pair
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