BDBM50315887 (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol::CHEMBL1091644::OSI-906

SMILES C[C@@]1(O)C[C@@H](C1)c1nc(-c2ccc3ccc(nc3c2)-c2ccccc2)c2c(N)nccn12

InChI Key InChIKey=PKCDDUHJAFVJJB-UHFFFAOYSA-N

Data  20 IC50  2 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 22 hits for monomerid = 50315887   

TargetInsulin receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 16nMAssay Description:Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 35nMAssay Description:Inhibition of human recombinant IGF-1R assessed as inhibition in the presence of ATP at 100 uM/l by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetInsulin receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 75nMAssay Description:Inhibition of recombinant human IR autophosphorylation using poly(Glu:Tyr) as substrate in presence of ATP by ELISA-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 35nMAssay Description:Inhibition of full-length human IGF1R autophosphorylation expressed in mouse NIH3T3 cells using poly(Glu:Tyr) as substrate in presence of ATP preincu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetATP-dependent translocase ABCB1(Human)
Rheinische Friedrich-Wilhelms-University of Bonn

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataEC50:  2.09E+3nMAssay Description:Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Human)
Rheinische Friedrich-Wilhelms-University of Bonn

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataEC50:  104nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as potentiation of SN-38-induced cytotoxic...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 24nMAssay Description:Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/19/2010
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/19/2010
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 18nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/19/2010
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 126nMAssay Description:Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 24nMAssay Description:Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 7.60nMAssay Description:Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 14nMAssay Description:Inhibition of IGF-1 receptor (unknown origin) in presence of [gamma33P]ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 34nMAssay Description:Inhibition of insulin receptor (unknown origin) in presence of [gamma33P]ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 2.80nMAssay Description:Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 st...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/13/2017
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 2nMAssay Description:Inhibition of IGF1R (unknown origin) using poly-G1 as substrate incubated for 10 mins prior to substrate addition measured after 1 hr by time-resolve...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2016
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 18nMAssay Description:Inhibition of recombinant INSR (unknown origin) using fluorescent dye-labelled KKSRGDYMTMQIG peptide peptide as substrate after 1 hr by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2015
Entry Details Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Vichem Chemie Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 1.25E+4nMAssay Description:Inhibition of recombinant c-MET (unknown origin) using poly-AEKY peptide as substrate after 60 mins by ADPGlo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2015
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 1.25E+4nMAssay Description:Inhibition of recombinant EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2015
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 12nMAssay Description:Inhibition of GST-tagged IGF-1R catalytic domain (unknown origin) using omnia Y peptide-12 as substrate assessed as inhibition of substrate phosphory...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Yangtze University

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50: 13nMAssay Description:Inhibition of GST-tagged IGF-1R catalytic domain (unknown origin) using omnia Y peptide-12 as substrate assessed as inhibition of substrate phosphory...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed