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-VLZXCDOPSA-N

Data  20 IC50  2 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 22 hits for monomerid = 50315887   

TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails PubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (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 EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Vichem Chemie 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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Vichem Chemie 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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Vichem Chemie 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 DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Vichem Chemie 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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Vichem Chemie Research

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 DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50:  35nMAssay Description:Compound was tested for the biological activity at the Beta-1 adrenergic receptorMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetInsulin receptor(Homo sapiens (Human))
Vichem Chemie Research

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50:  75nMAssay Description:Activity at beta-1 adrenergic receptorMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Osi Pharmaceuticals

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 DepthDetails ArticlePubMed