BindingDB PrimarySearch_ki

Found 89 with Last Name = 'calabrese' and Initial = 'm'

5'-AMP-activated protein kinase subunit beta-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

IC50: 400nMAssay Description:Activation of recombinant AMPKbeta1 in cryopreserved human hepatocytes assessed as reduction in 14C-2-acetic acid incorporation after 1 hr by scintil...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase subunit beta-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238079(US9394285, 173)

IC50: 420nMAssay Description:Activation of recombinant AMPKbeta1 in cryopreserved human hepatocytes assessed as reduction in 14C-2-acetic acid incorporation after 1 hr by scintil...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase subunit beta-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50463100(CHEMBL4249790)

IC50: 1.10E+4nMAssay Description:Activation of recombinant AMPKbeta1 in cryopreserved human hepatocytes assessed as reduction in 14C-2-acetic acid incorporation after 1 hr by scintil...More data for this Ligand-Target Pair

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3D Structure (crystal)

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

IC50: 1.40E+4nMAssay Description:Inhibition of PDE3A (unknown origin)More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase subunit beta-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50463101(CHEMBL4250253)

IC50: 2.50E+4nMAssay Description:Activation of recombinant AMPKbeta1 in cryopreserved human hepatocytes assessed as reduction in 14C-2-acetic acid incorporation after 1 hr by scintil...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM18137(AMP | CHEMBL752 | US11185100, TABLE 7.3 | [(2R,3S,...)

EC50: 1.52E+3nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 7nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM18137(AMP | CHEMBL752 | US11185100, TABLE 7.3 | [(2R,3S,...)

Kd: 3.70E+3nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237921(US9394285, 2)

Kd: 150nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase subunit gamma-1(Rattus norvegicus)
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 7nMAssay Description:Activation of recombinant rat AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphorylat...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: >4.00E+4nMAssay Description:Activation of recombinant human AMPK alpha2/beta2/gamma1 using Cy5-labelled SAMS as substrate in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 8.20nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 assessed as protection from Thr172 residue dephosphorylation preincubated for 15 mins follow...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 3.30nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 28nMAssay Description:Activation of recombinant human BAP-tagged AMPK alpha1/beta1/gamma1 assessed as protection from Thr172 residue dephosphorylation preincubated for 15 ...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-2/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: >4.00E+4nMAssay Description:Activation of recombinant human AMPK alpha1/beta2/gamma1 using Cy5-labelled SAMS as substrate in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM60978(6-Chloro-5-(4-methoxyphenyl)-1H-indazole-3-carboxy...)

EC50: 323nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237952(US9394285, 33)

EC50: 80nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237921(US9394285, 2)

EC50: 53nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50191352(CHEMBL3936376)

Kd: 9.95E+3nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237952(US9394285, 33)

Kd: 90nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237984(US9394285, 67)

Kd: 23nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-2/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 6.80nMAssay Description:Activation of recombinant human AMPK alpha2/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase subunit beta-2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: >4.00E+4nMAssay Description:Activation of recombinant human AMPK alpha2/beta2/gamma3 by using Cy5-labelled SAMS as substrate in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50191352(CHEMBL3936376)

EC50: 3.39E+3nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM60978(6-Chloro-5-(4-methoxyphenyl)-1H-indazole-3-carboxy...)

Kd: 1.78E+3nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237984(US9394285, 67)

EC50: 1.30nMAssay Description:Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphoryl...More data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

Kd: 9nMAssay Description:Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5-hydroxytryptamine receptor 2B(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: >3.00E+4nMAssay Description:Agonist activity at human recombinant 5-HT2b receptor expressed in CHO cells measured after 30 mins by HTRF assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237923(US9394285, 4)

Kd: 48nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237925(US9394285, 6)

Kd: 20nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238084(US9394285, 178 | US9394285, 179)

Kd: 14nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244636(CHEMBL4087189)

Kd: 1.70E+3nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244665(CHEMBL4097332)

Kd: 410nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

Kd: 9nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244667(CHEMBL4105032)

Kd: 14nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244665(CHEMBL4097332)

EC50: 270nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244668(CHEMBL4059813)

EC50: 62nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238084(US9394285, 178 | US9394285, 179)

EC50: 24nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237958(US9394285, 39)

EC50: 43nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238051(US9394285, 139)

EC50: 47nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237925(US9394285, 6)

EC50: 35nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237931(US9394285, 12)

EC50: 100nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244667(CHEMBL4105032)

EC50: 22nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237920(US9394285, 1)

EC50: 5.60nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244669(CHEMBL4079303)

EC50: 1.60E+3nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237931(US9394285, 12)

Kd: 48nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM237958(US9394285, 39)

Kd: 22nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

PDB Reactome pathway
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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM50244669(CHEMBL4079303)

Kd: 580nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238079(US9394285, 173)

Kd: 14nMAssay Description:Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL

PNG

BDBM238086(US9394285, 181)

EC50: 57nMAssay Description:Allosteric activation of human AMPK alpha1/beta1/gamma1 by TR-FRET assayMore data for this Ligand-Target Pair

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Filter my 89 hits

Targets 8▿
- 5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-1/subunit gamma-1 54
- 5'-AMP-activated protein kinase subunit gamma-1 8
- 5'-AMP-activated protein kinase catalytic subunit alpha-2/subunit beta-1/subunit gamma-1 7
- 5'-AMP-activated protein kinase catalytic subunit alpha-1/subunit beta-2/subunit gamma-1 7
- 5'-AMP-activated protein kinase subunit beta-2 7
- 5'-AMP-activated protein kinase subunit beta-1 4
- cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A 1
- 5-hydroxytryptamine receptor 2B 1
Publications 3▿
- J Med Chem 61: 7273-7288 (2018) 40
- J Med Chem 61: 2372-2383 (2018) 25
- J Med Chem 59: 8068-81 (2016) 24
Institutions 1▿
- Pfizer 89
Affinity: 1.3 to 4.0E+4 nM▿
- IC50 5
- Kd 24
- EC50 60
- Affinity ≤ nM
Xtal structures: 6
Docked structures: 0
Catalog Cmpds: 4