Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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 198062 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 198062 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 164124 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 164124 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 186635 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 186635 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 197761 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 197761 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 44320 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 44320 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 33982 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 33982 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 47824 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 47824 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 59871 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 59871 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 160984 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 160984 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 160984 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 160984 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 47825 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 47825 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 160984 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 160984 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 44915 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 44915 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 35027 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 35027 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 97984 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 97984 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 177914 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 177914 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 186021 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 186021 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 98201 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 98201 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 120335 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 120335 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 97408 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 97408 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 97786 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 97786 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 201643 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 201643 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 197751 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 197751 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 197900 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 197900 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 120275 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 120275 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 63430 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 63430 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 11286 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 11286 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 62435 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 62435 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 201918 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 201918 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 49232 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 49232 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 198104 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 198104 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 34083 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 34083 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 201788 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 201788 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 61977 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 61977 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 177705 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 177705 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 119490 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 119490 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 101478 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 101478 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 177831 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 177831 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 99362 47 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 99362 47 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 95395 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 95395 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 169190 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 169190 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 689 91 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
395 689 91 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
520 689 91 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 689 91 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 689 91 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 689 91 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 95489 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 95489 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 2699 57 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 2699 57 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 2699 57 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 2699 57 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 2699 57 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 177957 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 177957 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 186456 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 186456 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 899 13 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
515 899 13 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 899 13 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 899 13 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 10771 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 10771 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 163058 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 163058 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 197818 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 197818 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 899 13 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
515 899 13 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 899 13 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 899 13 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 117990 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 117990 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 163058 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 163058 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 61599 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 61599 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 899 13 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
515 899 13 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 899 13 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 899 13 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 111830 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 111830 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 201884 2 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 201884 2 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 899 13 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
515 899 13 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 899 13 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 899 13 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 102200 4 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 102200 4 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 177625 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 177625 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 10256 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 10256 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 118198 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 118198 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 201193 1 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 201193 1 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 120940 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 120940 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 94937 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 94937 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 155313 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 155313 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 197818 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 197818 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 94983 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 94983 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 177699 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 177699 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 186349 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 186349 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 46379 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 46379 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 10236 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 10236 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 201496 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 201496 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 102001 1 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 102001 1 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 121604 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 121604 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 9938 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 9938 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 34977 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 34977 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 2730 2 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 2730 2 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 2730 2 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 198320 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 198320 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 171789 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 171789 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 2924 55 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 2924 55 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 2924 55 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 2924 55 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 2924 55 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 94745 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 94745 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 178467 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 178467 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 186714 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 186714 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 10739 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 10739 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 156185 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 156185 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 99308 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 99308 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 177587 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 177587 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 185937 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 185937 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 171790 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 171790 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 10739 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 10739 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 59872 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 59872 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 3974 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 3974 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 4002 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 4002 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 107882 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 107882 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 198276 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 198276 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 171725 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 171725 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 65641 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 65641 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 171746 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 171746 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 118862 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 118862 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 198109 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 198109 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 34088 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 34088 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 35223 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 35223 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 97796 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 97796 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 201243 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 201243 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 44941 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 44941 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 197743 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 197743 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 120221 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 120221 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 114081 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 114081 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 95490 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 95490 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 198 10 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
480 198 10 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 198 10 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 94983 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 94983 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 2699 57 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 2699 57 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 2699 57 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 2699 57 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 2699 57 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 121758 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 121758 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 177815 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 177815 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 94982 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 94982 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 162578 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 162578 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 94983 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 94983 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 177625 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 177625 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 197812 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 197812 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 46563 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 46563 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 23239 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 23239 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 1230 39 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 1230 39 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 1230 39 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 34196 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 34196 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 118701 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 118701 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 162351 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 162351 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 97715 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 97715 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 121759 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 121759 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
5487 5576 53 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 Clc1ccc2nsnc2c1NC1=NCCN1 nan
CHEMBL1079 5576 53 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 Clc1ccc2nsnc2c1NC1=NCCN1 nan
44574138 177663 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 177663 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 183053 5 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 183053 5 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 177554 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 177554 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 121760 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 121760 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 155339 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 155339 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2924 55 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 2924 55 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 2924 55 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 2924 55 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 2924 55 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 177662 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 177662 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 177913 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 177913 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 186215 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 186215 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 95518 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 95518 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 28432 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 28432 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 28432 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 28432 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 34830 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 34830 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 62442 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 62442 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 107396 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 107396 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 49583 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 49583 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 12775 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 12775 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 12775 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 109922 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 109922 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 197120 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 197120 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 98957 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 98957 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 99239 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 99239 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 99295 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 99295 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 23239 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 23239 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 183053 5 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 183053 5 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 183053 5 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 183053 5 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 163329 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 163329 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 163329 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 163329 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 163329 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 163329 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 177625 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 177625 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 2730 2 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 2730 2 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 2730 2 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 97982 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 97982 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 154390 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 154390 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 154816 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 154816 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 183165 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 183165 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 154323 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 154323 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 44318 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 44318 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 185709 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 185709 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 121781 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 121781 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 94528 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 94528 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 167916 9 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 167916 9 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 99076 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 99076 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 2812 37 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 177785 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 177785 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 119417 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 119417 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 178466 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 178466 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 186399 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 186399 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 1318 55 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 1318 55 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 1318 55 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 1318 55 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 1318 55 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 118945 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 118945 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 94991 10 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 94991 10 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 34206 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 34206 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 111608 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 111608 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 196692 57 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 196692 57 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 97406 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 97406 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 201212 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 201212 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 186654 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 186654 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 167479 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 167479 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 10607 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 10607 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 10607 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 119148 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 119148 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 278 64 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 278 64 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
479 278 64 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 278 64 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 278 64 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 278 64 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 198280 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 198280 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 186381 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 186381 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 49514 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 49514 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 95413 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 95413 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 94743 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 94743 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 94743 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 94743 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 94743 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 94743 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 197697 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 197697 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 76480 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 76480 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 46758 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 46758 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 94527 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 94527 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 95022 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 95022 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 95022 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 95022 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 177700 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 177700 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 12958 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 12958 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 12958 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 171757 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 171757 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 186261 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 186261 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 10607 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 10607 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 10607 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 33533 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 33533 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 118655 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 118655 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 13404 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 13404 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 13404 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 115790 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 115790 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 115790 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 115790 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 198 10 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
480 198 10 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 198 10 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 10455 3 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 10455 3 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 10455 3 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 109902 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 109902 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 110062 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 110062 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 168462 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 168462 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 171846 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 171846 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 201666 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 201666 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 167210 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 167210 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 201225 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 201225 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 177592 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 177592 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 177832 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 177832 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 119416 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 119416 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 197734 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 197734 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 185821 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 185821 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 94744 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 94744 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 118872 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 118872 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 98986 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 98986 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 10455 3 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 10455 3 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 10455 3 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 186089 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 186089 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 183052 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 183052 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 9694 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 9694 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 110653 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 110653 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 58992 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 58992 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 64670 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 64670 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 46706 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 46706 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 110601 10 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 110601 10 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 121761 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 121761 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 177746 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 177746 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 178418 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 178418 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 185749 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 185749 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 9588 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 9588 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 10754 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 10754 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 59154 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 59154 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 2582 53 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 182787 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 182787 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 119020 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 119020 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 119347 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 119347 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 102300 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 102300 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 197752 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 197752 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 106785 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 106785 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 116078 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 116078 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 106785 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 106785 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 201702 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 201702 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 94936 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 94936 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 177584 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 177584 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 99435 5 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 99435 5 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 2363 19 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 2363 19 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 2363 19 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 2363 19 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 2363 19 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 177704 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 177704 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 120931 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 120931 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 177584 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 177584 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 177700 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 177700 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 94935 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 94935 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 94935 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 94935 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 61586 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 61586 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 201248 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 201248 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 60666 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 60666 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 164528 8 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
CHEMBL42359 164528 8 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
44574079 186478 0 None 8 2 Human 7.1 pEC50 = 7.1 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 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1