BDBM50116105 3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine::CHEMBL309138::R-121919::[3-(6-Dimethylamino-4-methyl-pyridin-3-yl)-2,5-dimethyl-4H-pyrazolo[1,5-a]pyrimidin-7-yl]-dipropyl-amine::[3-(6-Dimethylamino-4-methyl-pyridin-3-yl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-dipropyl-amine
SMILES: CCCN(CCC)c1cc(C)nc2c(c(C)nn12)-c1cnc(cc1C)N(C)C
InChI Key: InChIKey=ANNRUWYFVIGKHA-UHFFFAOYSA-N
Target/Host (Institution) | Ligand | Target/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 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Emory University Curated by ChEMBL | Assay Description Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting | Bioorg Med Chem Lett 25: 5111-4 (2015) BindingDB Entry DOI: 10.7270/Q2XW4MM0 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurogen Corporation Curated by ChEMBL | Assay Description Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells | Bioorg Med Chem Lett 18: 4486-90 (2008) Article DOI: 10.1016/j.bmcl.2008.07.063 BindingDB Entry DOI: 10.7270/Q2NG4RJ4 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | 3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Emory University Curated by ChEMBL | Assay Description Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin) | Bioorg Med Chem Lett 25: 5111-4 (2015) BindingDB Entry DOI: 10.7270/Q2XW4MM0 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurogen Corporation Curated by ChEMBL | Assay Description Antagonist activity at human CRF-1 receptor | J Med Chem 54: 4187-206 (2011) Article DOI: 10.1021/jm200365y BindingDB Entry DOI: 10.7270/Q2XS5VR1 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 3.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurocrine Biosciences, Inc. Curated by ChEMBL | Assay Description Inhibition of [125I]-o-CRF binding to CHO cells expressing human CRF1 receptor | J Med Chem 47: 4787-98 (2004) Article DOI: 10.1021/jm040058e BindingDB Entry DOI: 10.7270/Q2N29WDR | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor (Rattus norvegicus (rat)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 3.80 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurogen Corporation Curated by ChEMBL | Assay Description Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting | J Med Chem 54: 4187-206 (2011) Article DOI: 10.1021/jm200365y BindingDB Entry DOI: 10.7270/Q2XS5VR1 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 3.98 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurocrine Biosciences Curated by ChEMBL | Assay Description Antagonist activity at human recombinant CRF1 receptor | Bioorg Med Chem Lett 20: 7259-64 (2010) Article DOI: 10.1016/j.bmcl.2010.10.095 BindingDB Entry DOI: 10.7270/Q2736S5V | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | 5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurogen Corporation Curated by ChEMBL | Assay Description Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells | Bioorg Med Chem Lett 12: 2133-6 (2002) BindingDB Entry DOI: 10.7270/Q2SQ8ZPK | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 7.80 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Neurocrine Biosciences Curated by ChEMBL | Assay Description Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells | J Med Chem 48: 4100-10 (2005) Article DOI: 10.1021/jm050070m BindingDB Entry DOI: 10.7270/Q2ZK5HGJ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 8.30 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Eisai Co., Ltd. Curated by ChEMBL | Assay Description Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation | J Med Chem 55: 5255-69 (2012) Article DOI: 10.1021/jm300259r BindingDB Entry DOI: 10.7270/Q29P32XC | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 12 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. Curated by ChEMBL | Assay Description Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation | Bioorg Med Chem Lett 21: 6108-11 (2011) Article DOI: 10.1016/j.bmcl.2011.08.040 BindingDB Entry DOI: 10.7270/Q2F19046 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 8.5 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company Ltd. Curated by ChEMBL | Assay Description Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method | J Med Chem 59: 2551-66 (2016) BindingDB Entry DOI: 10.7270/Q24F1SNR | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 28.2 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline Medicines Research Centre Curated by ChEMBL | Assay Description Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells | J Med Chem 51: 7370-9 (2009) Article DOI: 10.1021/jm800744m BindingDB Entry DOI: 10.7270/Q2N87C1X | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 4 | n/a | n/a | n/a | n/a | n/a | n/a |
Eisai Co., Ltd. Curated by ChEMBL | Assay Description Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immu... | J Med Chem 55: 8450-63 (2012) Article DOI: 10.1021/jm300864p BindingDB Entry DOI: 10.7270/Q2KD202P | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Neurocrine Biosciences Inc. Curated by ChEMBL | Assay Description Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor | J Med Chem 48: 5104-7 (2005) Article DOI: 10.1021/jm050384+ BindingDB Entry DOI: 10.7270/Q2610ZVM | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 17 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company Ltd. Curated by ChEMBL | Assay Description Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas... | Bioorg Med Chem 25: 1556-1570 (2017) BindingDB Entry DOI: 10.7270/Q23R0W4P | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | 0.303 | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. Curated by ChEMBL | Assay Description Binding affinity to recombinant human CRF1 receptor expressed in CHO cells | Bioorg Med Chem Lett 21: 6108-11 (2011) Article DOI: 10.1016/j.bmcl.2011.08.040 BindingDB Entry DOI: 10.7270/Q2F19046 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | PubMed | n/a | n/a | 67 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceutical Company Ltd. Curated by ChEMBL | Assay Description Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 h... | Bioorg Med Chem 25: 1556-1570 (2017) BindingDB Entry DOI: 10.7270/Q23R0W4P | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Corticotropin releasing factor receptor 1 (Homo sapiens (Human)) | BDBM50116105 (3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Neurocrine Biosciences, Inc. Curated by ChEMBL | Assay Description Inhibition of [125I]-o-CRF binding to CHO cells expressing human CRF1 receptor | J Med Chem 47: 4787-98 (2004) Article DOI: 10.1021/jm040058e BindingDB Entry DOI: 10.7270/Q2N29WDR | |||||||||||
More data for this Ligand-Target Pair |