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LigandPNGBDBM50602306(CHEMBL5208487)
Affinity DataKi:  0.0260nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50149477(CHEMBL3770993 | US10851091, U.S. Pat. No. 8,242,10...)
Affinity DataKi:  0.0300nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM295665((S)-2-((2-((S)-4-(difluoromethyl)- 2-oxooxazolidin...)
Affinity DataKi:  0.0340nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
LigandPNGBDBM50602320(CHEMBL5199631)
Affinity DataKi:  0.0420nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM50602324(CHEMBL5198796)
Affinity DataKi:  0.0430nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM295669((S)-2-cyclopropyl-2-((2-((S)-4- (fluoromethyl)-2-o...)
Affinity DataKi:  0.0510nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50602323(CHEMBL5209168)
Affinity DataKi:  0.0530nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM475607(US10851091, Compound 103)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50602305(CHEMBL5209048)
Affinity DataKi:  0.0620nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
LigandPNGBDBM50602328(CHEMBL5205438)
Affinity DataKi:  0.0950nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM22000(7-[(3-hydroxypropyl)sulfanyl]-2-methyl-4-(2-methyl...)
Affinity DataKi:  0.0955nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602326(CHEMBL5181348)
Affinity DataKi:  0.0970nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged EGFR catalytic domain (669 to 1210 residues) expressed in baculovirus expression system by mass...More data for this Ligand-Target Pair
LigandPNGBDBM50149553(CHEMBL3770306)
Affinity DataKi:  0.100nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50317007(2-amino-4-(furan-2-yl)-5H-indeno[1,2-d]pyrimidin-5...)
Affinity DataKi:  0.100nMAssay Description:Antagonist activity at adenosine A2A receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50394718(CHEMBL2165801)
Affinity DataKi:  0.100nMAssay Description:Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602331(CHEMBL5182371)
Affinity DataKi:  0.100nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of wild-type EGFR (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
LigandPNGBDBM50149482(CHEMBL3770709)
Affinity DataKi:  0.100nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50161342(2-Amino-4-phenyl-indeno[1,2-d]pyrimidin-5-one | 2-...)
Affinity DataKi:  0.100nMAssay Description:Antagonist activity at adenosine A2A receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602304(CHEMBL5182339)
Affinity DataKi:  0.107nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50602321(CHEMBL5202305)
Affinity DataKi:  0.150nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50602329(CHEMBL5189517)
Affinity DataKi:  0.157nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM295676(US10851091, U.S. Pat. No. 8,242,104 No. 486 | US82...)
Affinity DataKi:  0.188nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetGlutamate carboxypeptidase 2(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM17659((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)
Affinity DataKi:  0.200nMAssay Description:In vitro inhibitory activity against glutamate carboxypeptidase II (GCP II) using N-acetyl-L-aspartyl-[3H]-L-glutamate as a substrateMore data for this Ligand-Target Pair
LigandPNGBDBM50149548(CHEMBL3771364 | US10851091, U.S. Pat. No. 8,242,10...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM50149483(CHEMBL3770325)
Affinity DataKi:  0.200nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50317008(2-amino-4-(5-chlorofuran-2-yl)-5H-indeno[1,2-d]pyr...)
Affinity DataKi:  0.200nMAssay Description:Antagonist activity at adenosine A2A receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate carboxypeptidase 2(Rat)
Zeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM17659((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)
Affinity DataKi:  0.275nMAssay Description:Compound was tested for inhibition of the Folate hydrolaseMore data for this Ligand-Target Pair
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM22001(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.275nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602325(CHEMBL5209394)
Affinity DataKi:  0.289nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetAdenosine receptor A2a(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50394722(CHEMBL2165807)
Affinity DataKi:  0.300nMAssay Description:Antagonist activity at human Adenosine receptor A2a assessed as inhibition of cAMP productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataKi:  0.300nMAssay Description:Inhibition of EGFR T790M/del746 to 750 mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
LigandPNGBDBM50149554(CHEMBL3770140)
Affinity DataKi:  0.300nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50434806(2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-y...)
Affinity DataKi:  0.300nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
LigandPNGBDBM50149476(CHEMBL3770717)
Affinity DataKi:  0.300nMAssay Description:Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM22001(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.302nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602313(CHEMBL5181675)
Affinity DataKi:  0.320nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50602332(CHEMBL5209238)
Affinity DataKi:  0.323nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM21986(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.330nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM21986(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.331nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50149548(CHEMBL3771364 | US10851091, U.S. Pat. No. 8,242,10...)
Affinity DataKi:  0.346nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50613695(CHEMBL5274166)
Affinity DataKi:  0.350nMAssay Description:Inhibition of human EGFR T790M/del (746 to 750 residues) mutant assessed as apparent inhibition constant using Fl-EEPLYWSFPAKKK-CONH2 peptide as subs...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM22002(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.355nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602308(CHEMBL5192172)
Affinity DataKi:  0.355nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMonocarboxylate transporter 1(Human)
Astrazeneca R&D Charnwood

Curated by ChEMBL
LigandPNGBDBM22002(5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methyl...)
Affinity DataKi:  0.355nMAssay Description:Displacement of [3H]5-[(3-hydroxypropyl)thio]-3-methyl-1-[2-(methyl-t)propyl-2,3-t2]-6-(1-naphthalenylmethyl)-1H-pyrrolo[3,4-d]pyrimidine-2,4(3H,6H)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A1(Human)
Johnson & Johnson Pharmaceutical Research and Development

Curated by ChEMBL
LigandPNGBDBM50317007(2-amino-4-(furan-2-yl)-5H-indeno[1,2-d]pyrimidin-5...)
Affinity DataKi:  0.400nMAssay Description:Antagonist activity at adenosine A1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50602315(CHEMBL5204346)
Affinity DataKi:  0.440nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
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