BDBM50443101 Cariprazine::RGH-188

SMILES CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(CC2)c2cccc(Cl)c2Cl)CC1

InChI Key InChIKey=KPWSJANDNDDRMB-UHFFFAOYSA-N

Data  55 KI  2 IC50  12 EC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 69 hits for monomerid = 50443101   

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Shanghai Jiao Tong University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataIC50: 2.07E+4nMAssay Description:Inhibition of recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential after 2 mins by patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  2.30nMAssay Description:Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  2.40nMAssay Description:Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  1nMAssay Description:Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissocia...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  0.400nMAssay Description:Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation prein...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  0.631nMAssay Description:Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  0.400nMAssay Description:Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation prein...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  0.180nMAssay Description:Partial agonist activity at human D2 receptor assessed as increase in cAMP accumulationMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  0.600nMAssay Description:Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  1nMAssay Description:Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissocia...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  110nMAssay Description:Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS bin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  3.5nMAssay Description:Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitmen...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataIC50: 1.70nMAssay Description:Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment aft...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataEC50:  5.80nMAssay Description:Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding a...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.0850nMAssay Description:Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.0850nMAssay Description:Displacement of [3H]Spiperone from dopamine D3 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Universidade De Santiago De Compostela

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.0850nMAssay Description:Partial agonist activity at human D3 receptor assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.0960nMAssay Description:Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes after 60 mins by scintillation counting metho...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2B(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.151nMAssay Description:Displacement of [3H]-5-HT from 5HT2B receptor in HEK293 cell membranes by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(3) dopamine receptor(Human)
Universidade De Santiago De Compostela

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.220nMAssay Description:Displacement of [3H]N-methylspiperone from human D3 receptor in HEK293 cell membranes measured after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(3) dopamine receptor(Human)
Universidade De Santiago De Compostela

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.269nMAssay Description:Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation c...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.270nMAssay Description:Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Friedrich-Alexander University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.270nMAssay Description:Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(3) dopamine receptor(Human)
Universidade De Santiago De Compostela

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.270nMAssay Description:Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation c...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.410nMAssay Description:Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.410nMAssay Description:Displacement of [3H]spiperone from human D2-short receptor expressed in CHO cell membranesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.470nMAssay Description:Displacement of [3H]spiperone from human D2-long receptor expressed in CHO cell membranesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.470nMAssay Description:Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.490nMAssay Description:Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.490nMAssay Description:Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.490nMAssay Description:Displacement of [3H]-spiperone from recombinant human D2L receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.501nMAssay Description:Modulation of human D2L receptorMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.690nMAssay Description:Displacement of [3H]Spiperone from human D2S receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  0.780nMAssay Description:Displacement of [3H]N-methylspiperone from human D2 receptor in HEK293 cell membranes measured after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]spiperone from recombinant human D2L receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  1.40nMAssay Description:Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scinti...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  1.5nMAssay Description:Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scinti...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  1.80nMAssay Description:Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in HEK293 cell membranes by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  2.60nMAssay Description:Displacement of [3H]OH-DPAT from recombinant human 5-HT1A receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  2.60nMAssay Description:Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  3.10nMAssay Description:Binding affinity to 5-HT1AR (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  3.10nMAssay Description:Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting metho...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation cou...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
National Institute On Drug Abuse?Intramural Research Program

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation cou...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Shanghaitech University

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  18nMAssay Description:Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO cell membranes after 3 hrs by liquid scintillation counting analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Shanghai Institute of Pharmaceutical Industry

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Shanghai Institute of Pharmaceutical Industry

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in rat cortex tissue incubated for 30 mins by liquid scintillation counting meth...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Shanghai Institute of Pharmaceutical Industry

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  22nMAssay Description:Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293T cell membranesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Shanghai Institute of Pharmaceutical Industry

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  22nMAssay Description:Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 cells by competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
Shanghai Institute of Pharmaceutical Industry

Curated by ChEMBL
LigandPNGBDBM50443101(Cariprazine | RGH-188)
Affinity DataKi:  23nMAssay Description:Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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