BDBM31592 PF-2545920::US9138494, MP-10::substituted pyrazole, 9

SMILES Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1

InChI Key InChIKey=AZEXWHKOMMASPA-UHFFFAOYSA-N

Data  1 KI  15 IC50  3 Kd

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 19 hits for monomerid = 31592   

TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataKi:  0.170nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
TargetGalectin-3(Homo sapiens (Human))
Stanford University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataKd:  290nMAssay Description:Binding affinity to recombinant human galectin 3 assessed as dissociation constant by SPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.646nMAssay Description:Inhibition of rat recombinant PDE10A expressed in baculovirus infected Sf9 cells using [3H]cAMP as substrate after 60 mins by TopCount scintillation ...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of full-length human recombinant PDE10A using cyclic AMP as substrate by scintillation proximity assayMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.370nMAssay Description:Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step r...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of PDE10A (unknown origin)More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.180nMAssay Description:Binding affinity to PDE10A (unknown origin)More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillatio...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of PDE10AMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of rat PDE10AMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of PDE10AMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.501nMAssay Description:Inhibition of rat recombinant PDE10A expressed in baculovirus infected insect Sf9 cells using [3H]cAMP as substrate after 60 mins by scintillation co...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.5nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of PDE10A (unknown origin)More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.370nMAssay Description:Inhibition of human PDE10A2 catalytic domain (446 to 789 residues) expressed in Escherichia coli BL21 cells using [3H]-cGMP as substrate after 15 min...More data for this Ligand-Target Pair
TargetGalectin-3(Homo sapiens (Human))
Stanford University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataKd:  150nMAssay Description:Binding affinity to recombinant human galectin 3 assessed as dissociation constant by fluorescent anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGalectin-1(Homo sapiens (Human))
Stanford University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataKd: >5.00E+5nMAssay Description:Binding affinity to recombinant human galectin 1 assessed as dissociation constant by fluorescent anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.370nMpH: 7.5 T: 2°CAssay Description:PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  1.68nMAssay Description:The PDE enzymatic reaction was carried out in assay buffer (20 mM Tris-HCl pH7.5, 10 mM MgCl2, 0.1% bovine serum albumin) containing enzyme and subst...More data for this Ligand-Target Pair