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TargetThrombospondin-1(Human)
Daiichi Sankyo

US Patent
LigandPNGBDBM521738(US11149066, Compound 13)
Affinity DataKd:  0.0960nMAssay Description:As referred to herein, the TSP1 inhibitory activity refers to the activity to inhibit one or more effects of TSP1, including angiostatic effect. The ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2022
Entry Details
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TargetBeta-3 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259321((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50:  280nMAssay Description:Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259469((S)-N-Propyl-4'-{2-[(2-hydroxy-3-phenoxypropyl)-am...)
Affinity DataEC50:  500nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRetinoic acid receptor RXR-alpha(Human)
Okayama University

Curated by ChEMBL
LigandPNGBDBM50325037(6-(ethyl(8-methyl-7-oxo-5-(trifluoromethyl)-7,8-di...)
Affinity DataEC50:  1.00E+3nMAssay Description:Agonist activity at human RXRalpha expressed in human COS7 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392657(US10301286, Example 5)
Affinity DataEC50:  25nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392670(US10301286, Example 24)
Affinity DataEC50:  3.20nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392682(US10301286, Example 68)
Affinity DataEC50:  530nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetThrombospondin-1(Human)
Daiichi Sankyo

US Patent
LigandPNGBDBM521734(US11149066, Compound 9)
Affinity DataKd:  0.230nMAssay Description:As referred to herein, the TSP1 inhibitory activity refers to the activity to inhibit one or more effects of TSP1, including angiostatic effect. The ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2022
Entry Details
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TargetRetinoic acid receptor RXR-alpha(Human)
Okayama University

Curated by ChEMBL
LigandPNGBDBM50429866(CHEMBL2332887)
Affinity DataEC50:  15nMAssay Description:Partial agonist activity at RXRalpha (unknown origin) expressed in COS1 cells after 18 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392659(US10301286, Example 11)
Affinity DataEC50:  17nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392666(US10301286, Example 16 | US10301286, Example 15)
Affinity DataEC50:  490nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetBeta-2 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259252((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392674(US10301286, Example 35)
Affinity DataEC50:  140nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMelanocortin receptor 3(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392681(US10301286, Example 57)
Affinity DataEC50:  2.40E+3nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMetabotropic glutamate receptor 2(Human)
Taisho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50094844((+/-)-2-Amino-6-methyl-bicyclo[3.1.0]hexane-2,6-di...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50457784(CHEMBL4204089)
Affinity DataEC50: >1.00E+6nMAssay Description:Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetMelanocyte-stimulating hormone receptor(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392656(US10301286, Example 4)
Affinity DataEC50:  70nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392671(US10301286, Example 27)
Affinity DataEC50:  1.00E+3nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
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TargetMetabotropic glutamate receptor 3(Rat)
Taisho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50056272((2S,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxy...)
Affinity DataEC50:  62.8nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 3More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMetabotropic glutamate receptor 3(Rat)
Taisho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50094841(2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarbox...)
Affinity DataEC50:  45.4nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 3More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetMelanocyte-stimulating hormone receptor(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392685(US10301286, Example 74)
Affinity DataEC50:  1.40E+3nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

LigandPNGBDBM50318885(teriparatide | CHEMBL525610)
Affinity DataEC50:  2.5nMAssay Description:Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetBeta-3 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259205((S)-4'-(2-{[2-Hydroxy-3-(carbazol-4-yloxy)propyl]-...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259252((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50:  2.50E+3nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetVitamin D3 receptor(Human)
Teikyo University

Curated by ChEMBL
LigandPNGBDBM50437335(CHEMBL2407824)
Affinity DataEC50:  0.0440nMAssay Description:Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetRetinoic acid receptor RXR-alpha(Human)
Okayama University

Curated by ChEMBL
LigandPNGBDBM50391814(CHEMBL2146901)
Affinity DataEC50:  143nMAssay Description:Partial agonist activity at RXRalpha (unknown origin) expressed in COS1 cells after 18 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetMelanocortin receptor 3(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392658(US10301286, Example 9)
Affinity DataEC50:  910nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMelanocortin receptor 3(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392685(US10301286, Example 74)
Affinity DataEC50:  1.00E+3nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392665(US10301286, Example 13)
Affinity DataEC50:  48nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetThrombospondin-1(Human)
Daiichi Sankyo

US Patent
LigandPNGBDBM521737(US11149066, Compound 12)
Affinity DataKd:  0.380nMAssay Description:As referred to herein, the TSP1 inhibitory activity refers to the activity to inhibit one or more effects of TSP1, including angiostatic effect. The ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2022
Entry Details
Go to US Patent

TargetBeta-2 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259364((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259124((S)-4'-(2-{[2-Hydroxy-3-(carbazol-4-yloxy)propyl]-...)
Affinity DataEC50:  1.30E+3nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocortin receptor 3(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392672(US10301286, Example 28)
Affinity DataEC50:  1.00E+4nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259255((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50:  180nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocyte-stimulating hormone receptor(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392660(US10301286, Example 76)
Affinity DataEC50:  100nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetBeta-3 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM25392(Isoproterenol,(+) | CHEMBL434 | 4-[1-hydroxy-2-(pr...)
Affinity DataEC50:  12nMAssay Description:Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392662(US10301286, Example 88)
Affinity DataEC50:  12nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMelanocyte-stimulating hormone receptor(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392672(US10301286, Example 28)
Affinity DataEC50:  3.90E+3nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetBeta-2 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259124((S)-4'-(2-{[2-Hydroxy-3-(carbazol-4-yloxy)propyl]-...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392681(US10301286, Example 57)
Affinity DataEC50:  120nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMetabotropic glutamate receptor 2(Human)
Taisho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50094848((1S,2S,3R,5R,6S)-2-amino-3-fluorobicyclo[3.1.0]hex...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259167((S)-4'-(2-{[2-Hydroxy-3-(indol-4-yloxy)propyl]amin...)
Affinity DataEC50:  280nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-2 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259321((S)-4'-{2-[(2-Hydroxy-3-phenoxypropyl)amino]ethyl}...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-3 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259124((S)-4'-(2-{[2-Hydroxy-3-(carbazol-4-yloxy)propyl]-...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetThrombospondin-1(Human)
Daiichi Sankyo

US Patent
LigandPNGBDBM521727(US11149066, Compound 1)
Affinity DataKd:  0.510nMAssay Description:As referred to herein, the TSP1 inhibitory activity refers to the activity to inhibit one or more effects of TSP1, including angiostatic effect. The ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2022
Entry Details
Go to US Patent

TargetBeta-1 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259205((S)-4'-(2-{[2-Hydroxy-3-(carbazol-4-yloxy)propyl]-...)
Affinity DataEC50:  250nMAssay Description:Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMetabotropic glutamate receptor 2(Human)
Taisho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50279772(2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cy...)
Affinity DataEC50:  50.3nMAssay Description:Antagonist activity against Metabotropic glutamate receptor 2
expressed in CHO cells was evaluated in presence of 30 uM glutamic acid
More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetBeta-2 adrenergic receptor(Human)
Astellas Pharma

Curated by ChEMBL
LigandPNGBDBM50259468((S)-N-Methyl-4'-{2-[(2-hydroxy-3-phenoxypropyl)-am...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetMelanocyte-stimulating hormone receptor(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392658(US10301286, Example 9)
Affinity DataEC50:  390nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

TargetMelanocortin receptor 4(Human)
Astellas Pharma

US Patent
LigandPNGBDBM392677(US10301286, Example 47)
Affinity DataEC50:  62nMAssay Description:Experiment Method(1) Construction of Human MC Receptor-Expressing VectorA human MC4 receptor gene (GenBank Accession No.: NM_005912.2), a human MC1 r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2020
Entry Details
Go to US Patent

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