Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10934575 202781 0 None 3 5 Human 10.0 pEC50 = 10.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 202781 0 None 3 5 Human 10.0 pEC50 = 10.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
44362146 164382 1 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL422477 164382 1 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44574074 188879 0 None 977 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513691 188879 0 None 977 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
11109088 202479 0 None 1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 202479 0 None 1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
22493318 44504 0 None 13 3 Human 9.3 pEC50 = 9.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL152155 44504 0 None 13 3 Human 9.3 pEC50 = 9.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44362194 34159 1 None 10 3 Human 9.3 pEC50 = 9.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142784 34159 1 None 10 3 Human 9.3 pEC50 = 9.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493352 48010 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155326 48010 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
22493236 60077 0 None 5 3 Human 9.1 pEC50 = 9.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL17491 60077 0 None 5 3 Human 9.1 pEC50 = 9.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44271661 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL414185 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44271661 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL414185 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493280 48011 0 None 1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155327 48011 0 None 1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44271661 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL414185 161247 0 None -1 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44369431 45099 0 None 57 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL152693 45099 0 None 57 3 Human 9.1 pEC50 = 9.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44362208 35205 1 None 3 3 Human 9.0 pEC50 = 9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143801 35205 1 None 3 3 Human 9.0 pEC50 = 9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493258 98211 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL277375 98211 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44574078 178184 0 None 120 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468711 178184 0 None 120 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44219718 188259 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL506744 188259 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44362286 98429 1 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL279136 98429 1 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362195 120576 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL357129 120576 0 None 2 3 Human 8.9 pEC50 = 8.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493263 97633 0 None 50 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL273316 97633 0 None 50 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493365 98012 0 None 15 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL275844 98012 0 None 15 3 Human 8.9 pEC50 = 8.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44329788 206362 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97859 206362 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
11098175 202469 0 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 202469 0 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
10221005 202619 0 None 72 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 202619 0 None 72 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44362185 120516 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL356605 120516 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493343 63640 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18069 63640 0 None 19 3 Human 8.7 pEC50 = 8.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44343410 11450 2 None -1 3 Human 8.0 pEC50 = 8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL118055 11450 2 None -1 3 Human 8.0 pEC50 = 8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9837963 62642 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17851 62642 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329796 206638 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99559 206638 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493289 49420 0 None 4 3 Human 8.0 pEC50 = 8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL156661 49420 0 None 4 3 Human 8.0 pEC50 = 8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
11034737 202823 0 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 202823 0 None -1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44362145 34260 3 None - 1 Human 7.0 pEC50 = 7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142864 34260 3 None - 1 Human 7.0 pEC50 = 7 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493401 206508 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98769 206508 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493225 62183 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17819 62183 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
44574878 177972 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL466916 177972 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
22493372 119733 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL352225 119733 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
11059195 101702 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL302698 101702 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44574987 178101 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467915 178101 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
76632 99588 48 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
CHEMBL287047 99588 48 None -5 2 Human 5.0 pEC50 = 5.0 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
44449657 95620 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260009 95620 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571891 169449 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL444252 169449 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
2435 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 714 98 None -14 8 Bovine 6.0 pEC50 = 6.0 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
44449690 95714 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
CHEMBL260575 95714 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
1960 2815 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2815 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2815 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2815 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2815 64 None -199 13 Rat 5.9 pEC50 = 5.9 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
44574105 178230 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL469127 178230 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44574045 188697 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
CHEMBL512062 188697 0 None 60 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
2765 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
515 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
CHEMBL13852 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
DB09202 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
22493274 10935 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117581 10935 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
10015132 163317 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
CHEMBL420683 163317 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
9817256 202536 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL71001 202536 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
2765 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
515 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
CHEMBL13852 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
DB09202 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
10038958 118220 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL341747 118220 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
10015132 163317 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL420683 163317 1 None 29 3 Human 7.9 pEC50 = 7.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
22493265 61805 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17776 61805 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
2765 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
515 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
CHEMBL13852 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
DB09202 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
44329790 112054 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329928 112054 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493224 206604 4 None 6 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99362 206604 4 None 6 3 Human 7.9 pEC50 = 7.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
2765 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
515 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
CHEMBL13852 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
DB09202 930 16 None 5 7 Human 7.9 pEC50 = 7.9 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
12924821 102424 5 None - 1 Human 6.9 pEC50 = 6.9 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
CHEMBL30596 102424 5 None - 1 Human 6.9 pEC50 = 6.9 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
44593577 177889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
44343251 10420 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL116843 10420 2 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
44362510 118428 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL342324 118428 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
22493257 205912 3 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95245 205912 3 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
44362289 121183 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL358802 121183 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
44449306 95162 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257801 95162 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449730 155567 0 None 22 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL406316 155567 0 None 22 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
9817256 202536 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 202536 0 None 251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44449278 95208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44574877 177966 0 None 23 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466869 177966 0 None 23 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44574135 188589 0 None 18 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL511211 188589 0 None 18 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
22493269 46563 0 None 6 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154023 46563 0 None 6 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44343257 10400 0 None 13 3 Human 7.8 pEC50 = 7.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL116700 10400 0 None 13 3 Human 7.8 pEC50 = 7.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
10199052 206215 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97044 206215 0 None 5 3 Human 7.8 pEC50 = 7.8 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
619552 102225 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL304747 102225 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
45280075 121848 0 None -91 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3600395 121848 0 None -91 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44343235 10102 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL115977 10102 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44362013 35156 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
CHEMBL143766 35156 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
481 2848 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
9838763 2848 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
CHEMBL72958 2848 5 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
10199335 203039 0 None 120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 203039 0 None 120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44574834 172052 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
CHEMBL449279 172052 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
2146 3051 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3051 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3051 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3051 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3051 63 None -281 10 Rat 5.8 pEC50 = 5.8 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44449247 94970 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256984 94970 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571843 178741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473425 178741 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571937 188959 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL514333 188959 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
9794803 10903 2 None 4 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL117381 10903 2 None 4 3 Human 7.8 pEC50 = 7.8 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449692 156443 0 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL407308 156443 0 None 8 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
44281493 99534 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
CHEMBL286702 99534 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
44574106 177851 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466012 177851 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574107 188174 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL505414 188174 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
44574935 172053 0 None 19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL449284 172053 0 None 19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
9794803 10903 2 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117381 10903 2 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9859855 60078 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17492 60078 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
124 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
2032 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
4636 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
CHEMBL762 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
DB00935 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
22493320 4140 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100198 4140 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329481 4168 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100383 4168 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10378649 108106 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL320419 108106 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
124 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
2032 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
4636 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
CHEMBL762 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
DB00935 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
11811395 202995 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74071 202995 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44571844 171987 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL448510 171987 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493367 65854 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18436 65854 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44574075 172008 0 None 72 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448802 172008 0 None 72 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
44369351 119097 0 None 2 3 Human 8.7 pEC50 = 8.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL346380 119097 0 None 2 3 Human 8.7 pEC50 = 8.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
11140347 202828 0 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 202828 0 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44362196 34265 1 None 7 3 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142871 34265 1 None 7 3 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362288 35401 1 None 251 2 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143973 35401 1 None 251 2 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
9881853 98022 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275902 98022 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10198532 205962 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95523 205962 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44369434 45125 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL152725 45125 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
9947861 202461 0 None 21 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 202461 0 None 21 3 Human 8.6 pEC50 = 8.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
124 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 2933 44 None -26 21 Human 7.7 pEC50 = 7.7 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
10422033 120462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL356195 120462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281250 114308 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
CHEMBL33405 114308 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
44449691 95715 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL260576 95715 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
4038180 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None -2 5 Human 7.7 pEC50 = 7.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
44449278 95208 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95208 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
1960 2815 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2815 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2815 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2815 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2815 64 None -23 13 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
10135864 122003 0 None -10 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601200 122003 0 None -10 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44574937 178085 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467688 178085 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
44449276 95207 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257976 95207 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
11090351 162839 0 None 20 2 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 162839 0 None 20 2 Human 7.6 pEC50 = 7.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
44449278 95208 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95208 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44593577 177889 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177889 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
10221004 202530 0 None 20 2 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 202530 0 None 20 2 Human 6.6 pEC50 = 6.6 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
22493356 46747 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154170 46747 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10804826 23412 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23412 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
216249 1278 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
3469 1278 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
CHEMBL257978 1278 44 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
10423384 34373 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
CHEMBL142958 34373 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
10084685 118931 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL344957 118931 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
10221066 162612 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL417999 162612 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44271931 97941 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275386 97941 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10180440 122004 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601201 122004 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
2683 3774 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
5487 3774 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
7308 3774 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
CHEMBL1079 3774 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
DB00697 3774 57 None -1 3 Bovine 6.6 pEC50 = 6.6 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
44574138 177930 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466635 177930 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
44593557 183336 7 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL481322 183336 7 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44574874 177818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL465599 177818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
122184771 122005 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601202 122005 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44449723 155593 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL406348 155593 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
124 2933 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2933 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2933 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2933 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2933 44 None -52 21 Rat 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2146 3051 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3051 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3051 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3051 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3051 63 None -35 10 Human 5.5 pEC50 = 5.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44574134 177929 0 None 91 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466634 177929 0 None 91 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574077 178183 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468710 178183 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
44574136 188454 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL509350 188454 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44449725 95743 0 None 208 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260720 95743 0 None 208 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44269124 28605 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL13789 28605 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
44269124 28605 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL13789 28605 1 None 23 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
10060965 35008 1 None 39 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL143562 35008 1 None 39 3 Human 8.5 pEC50 = 8.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816515 62649 0 None 5 3 Human 8.5 pEC50 = 8.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17856 62649 0 None 5 3 Human 8.5 pEC50 = 8.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44329797 107620 0 None 67 3 Human 8.5 pEC50 = 8.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL319553 107620 0 None 67 3 Human 8.5 pEC50 = 8.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10244367 49773 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL156950 49773 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11000184 12941 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 12941 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 12941 0 None 4 5 Human 8.5 pEC50 = 8.5 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
44343247 110146 0 None 15 3 Human 8.4 pEC50 = 8.4 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL325745 110146 0 None 15 3 Human 8.4 pEC50 = 8.4 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
15959112 201838 0 None -1 2 Rat 5.5 pEC50 = 5.5 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL66433 201838 0 None -1 2 Rat 5.5 pEC50 = 5.5 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
11264016 99185 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
CHEMBL284307 99185 2 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
44281507 99465 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
CHEMBL286226 99465 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
44280965 99521 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
CHEMBL286609 99521 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
10804826 23412 1 None -1 2 Rat 4.5 pEC50 = 4.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23412 1 None -1 2 Rat 4.5 pEC50 = 4.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
44593557 183336 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
CHEMBL481322 183336 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
44593557 183336 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481322 183336 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9816986 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL421011 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
9816986 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL421011 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816986 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL421011 163587 0 None 21 3 Human 7.5 pEC50 = 7.5 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44593577 177889 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 177889 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
481 2848 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
9838763 2848 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
CHEMBL72958 2848 5 None 8 2 Human 6.5 pEC50 = 6.5 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
22493344 98209 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL277361 98209 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44449277 154644 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402388 154644 2 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449305 155070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL404566 155070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571889 183447 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
CHEMBL482148 183447 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
44449337 154577 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402003 154577 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
22493272 44502 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
CHEMBL152154 44502 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
44574133 187792 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL501404 187792 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
122184835 122026 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601310 122026 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44449249 94754 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255938 94754 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10420352 168175 10 None -83 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168175 10 None -83 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
44280982 99303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
CHEMBL285082 99303 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
124 2933 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2933 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2933 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2933 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2933 44 None -26 21 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
44574936 178054 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL467495 178054 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44369646 119658 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
CHEMBL351543 119658 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
44571841 178740 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473424 178740 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44574988 188640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511576 188640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
521 1377 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
5311068 1377 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
835 1377 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
CHEMBL778 1377 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
DB00633 1377 64 None -104 4 Bovine 6.4 pEC50 = 6.4 Functional
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
22493349 119182 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
CHEMBL347268 119182 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
17804479 95216 16 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258007 95216 16 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10083742 34383 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL142967 34383 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
44329739 111832 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329272 111832 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
104452 201412 66 None -4 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL63976 201412 66 None -4 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
22493381 97631 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
CHEMBL273312 97631 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
22493231 205931 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95333 205931 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
44574104 188899 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513871 188899 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
9838376 167737 0 None 15 2 Human 8.4 pEC50 = 8.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
CHEMBL434074 167737 0 None 15 2 Human 8.4 pEC50 = 8.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
11108001 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
9816460 119388 0 None 39 3 Human 8.3 pEC50 = 8.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL349082 119388 0 None 39 3 Human 8.3 pEC50 = 8.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
1028 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 287 69 None -10 16 Human 6.4 pEC50 = 6.4 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
11058166 202999 0 None 10 2 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 202999 0 None 10 2 Human 7.4 pEC50 = 7.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
44574986 188621 0 None 7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511411 188621 0 None 7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
22493415 49703 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL156893 49703 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
44449686 95638 0 None 7 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL260116 95638 0 None 7 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
25066019 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256982 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
25066019 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL256982 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
25066019 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL256982 94968 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
11079593 202415 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70326 202415 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
15959119 76703 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL207277 76703 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
44369647 46943 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL154346 46943 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449248 94753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255937 94753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95247 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258178 95247 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95247 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL258178 95247 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44593580 177967 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 177967 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
11747739 13124 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1191324 13124 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL542402 13124 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574103 172019 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448908 172019 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574137 188501 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL510023 188501 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
11108001 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117248 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL540542 10771 2 None -2 5 Human 8.3 pEC50 = 8.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44362149 33710 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142387 33710 0 None 2 3 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362150 118885 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL344551 118885 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
10859076 13570 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 13570 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 13570 0 None 5 4 Human 8.3 pEC50 = 8.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
6604803 116018 2 None 1 4 Rat 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116018 2 None 1 4 Rat 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
6604803 116018 2 None -1 4 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116018 2 None -1 4 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
4038180 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 202 11 None 1 5 Rat 8.2 pEC50 = 8.2 Functional
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
9816461 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117094 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL544290 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44343245 110126 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL325648 110126 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44343275 110285 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL326067 110285 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
22493233 168721 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
CHEMBL441412 168721 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
9903313 172109 0 None 5 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL450018 172109 0 None 5 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493379 206385 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98016 206385 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493411 167467 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL432192 167467 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329701 205944 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95398 205944 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44574044 177856 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL466046 177856 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44219719 178102 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467916 178102 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
10399043 119657 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL351542 119657 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10916464 202452 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70563 202452 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
44574875 188058 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL503269 188058 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
44449245 94969 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL256983 94969 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
22493347 119107 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL346465 119107 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281057 99214 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
CHEMBL284486 99214 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
9816461 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 10619 6 None 60 2 Human 7.3 pEC50 = 7.3 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574938 188327 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL507755 188327 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
44571888 183335 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481321 183335 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343244 9858 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114669 9858 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
44343236 110876 0 None 15 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL327005 110876 0 None 15 3 Human 8.2 pEC50 = 8.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9903932 59198 0 None 501 2 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17151 59198 0 None 501 2 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44271932 64880 0 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18256 64880 0 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493392 46891 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL154298 46891 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
9838192 110824 13 None -2 3 Rabbit 7.2 pEC50 = 7.2 Functional
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
CHEMBL326702 110824 13 None -2 3 Rabbit 7.2 pEC50 = 7.2 Functional
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
122184772 122006 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601203 122006 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44574132 178014 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL467259 178014 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44571842 178692 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473043 178692 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571887 187832 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL502078 187832 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343243 9752 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114054 9752 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
44343173 10918 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL117482 10918 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9838294 59361 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17221 59361 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
11079 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
3369 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
4436 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
5509 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
CHEMBL761 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
DB06711 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
11079 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
3369 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
4436 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
5509 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
CHEMBL761 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
DB06711 2693 59 None -1 3 Human 7.2 pEC50 = 7.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
25154770 183070 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL480272 183070 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493325 119257 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL347920 119257 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
22493287 119588 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL350906 119588 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11097789 102524 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 102524 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
11140345 202470 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 202470 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
9795167 107008 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL318544 107008 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44352155 116308 0 None 7 5 Human 8.1 pEC50 = 8.1 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL337862 116308 0 None 7 5 Human 8.1 pEC50 = 8.1 Functional
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
9795167 107008 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL318544 107008 0 None 6 3 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329703 206421 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98243 206421 0 None 7 2 Human 8.1 pEC50 = 8.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44449304 95161 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257800 95161 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
12764879 177848 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 177848 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
172745 99661 7 None -234 2 Human 4.2 pEC50 = 4.2 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL287587 99661 7 None -234 2 Human 4.2 pEC50 = 4.2 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
1753 2468 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
483 2468 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
6082 2468 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
CHEMBL524 2468 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
DB00723 2468 26 None -12 2 Human 6.1 pEC50 = 6.1 Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
12764880 177971 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466914 177971 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
22493359 121174 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
CHEMBL358685 121174 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
12764879 177848 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 177848 0 None 100 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44593580 177967 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 177967 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44449303 95160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257799 95160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449303 95160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL257799 95160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9840212 61792 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17764 61792 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329133 205967 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95565 205967 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493408 60871 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17657 60871 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
541604 164787 10 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019