Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL836 ada1a_human Human Yes 10.2 EC50 = 0.1 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C
CHEMBL72441 ada1a_human Human No 10.0 EC50 = 0.1 nM Funct
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
235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1
CHEMBL422477 ada1a_human Human Yes 9.6 EC50 = 0.3 nM Funct
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
258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1
CHEMBL513691 ada1a_human Human No 9.4 EC50 = 0.4 nM Funct
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
262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1
CHEMBL70751 ada1a_human Human No 9.4 EC50 = 0.4 nM Funct
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
255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1
CHEMBL152155 ada1a_human Human No 9.3 EC50 = 0.5 nM Funct
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
241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1
CHEMBL142784 ada1a_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1
CHEMBL155326 ada1a_human Human No 9.2 EC50 = 0.7 nM Funct
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
242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1
CHEMBL17491 ada1a_human Human No 9.1 EC50 = 0.8 nM Funct
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
242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1
CHEMBL414185 ada1a_human Human No 9.1 EC50 = 0.8 nM Funct
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.
233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1
CHEMBL414185 ada1a_human Human No 9.1 EC50 = 0.8 nM Funct
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
233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1
CHEMBL155327 ada1a_human Human No 9.1 EC50 = 0.8 nM Funct
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
242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1
CHEMBL414185 ada1a_human Human No 9.1 EC50 = 0.8 nM Funct
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
233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1
CHEMBL152693 ada1a_human Human No 9.1 EC50 = 0.9 nM Funct
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
271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1
CHEMBL143801 ada1a_human Human Yes 9.0 EC50 = 1 nM Funct
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
258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1
CHEMBL277375 ada1a_human Human No 9.0 EC50 = 1 nM Funct
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
241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1
CHEMBL468711 ada1a_human Human No 9.0 EC50 = 1 nM Funct
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
261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1
CHEMBL506744 ada1a_human Human No 9.0 EC50 = 1 nM Funct
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
280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1
CHEMBL279136 ada1a_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1
CHEMBL357129 ada1a_human Human No 8.9 EC50 = 1.3 nM Funct
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
241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1
CHEMBL273316 ada1a_human Human No 8.9 EC50 = 1.3 nM Funct
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
270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL275844 ada1a_human Human No 8.9 EC50 = 1.3 nM Funct
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
241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1
CHEMBL97859 ada1a_human Human No 8.9 EC50 = 1.3 nM Funct
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.
275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1
CHEMBL70691 ada1a_human Human No 8.8 EC50 = 1.6 nM Funct
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
251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1
CHEMBL71479 ada1a_human Human No 8.7 EC50 = 2.0 nM Funct
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
267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1
CHEMBL356605 ada1a_human Human No 8.7 EC50 = 2.0 nM Funct
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
253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1
CHEMBL18069 ada1a_human Human No 8.7 EC50 = 2.0 nM Funct
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
256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL118055 ada1a_human Human Yes 8.0 EC50 = 10 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1
CHEMBL17851 ada1a_human Human No 8.0 EC50 = 10 nM Funct
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
255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1
CHEMBL99559 ada1a_human Human No 8.0 EC50 = 10 nM Funct
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.
275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1
CHEMBL156661 ada1a_human Human No 8.0 EC50 = 10 nM Funct
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
253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1
CHEMBL72724 ada1a_human Human No 8.0 EC50 = 10.5 nM Funct
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
289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1
CHEMBL142864 ada1a_human Human Yes 7.0 EC50 = 100 nM Funct
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
242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1
CHEMBL98769 ada1a_human Human No 7.0 EC50 = 100 nM Funct
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.
288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL17819 ada1a_human Human No 6.0 EC50 = 1000 nM Funct
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
270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1
CHEMBL466916 ada1a_human Human No 6.0 EC50 = 1050 nM Funct
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
228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1
CHEMBL352225 ada1a_human Human No 7.0 EC50 = 109.7 nM Funct
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
256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1
CHEMBL302698 ada1a_human Human No 6.0 EC50 = 1096.5 nM Funct
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
321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1
CHEMBL467915 ada1a_human Human No 8.0 EC50 = 11 nM Funct
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
250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1
CHEMBL3947830 ada1a_human Human No 8.0 EC50 = 11.1 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
484 10 1 5 4.3 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1
CHEMBL287047 ada1a_human Human Yes 5.0 EC50 = 11000 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1
CHEMBL260009 ada1a_human Human No 7.0 EC50 = 111 nM Funct
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
265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1
CHEMBL444252 ada1a_human Human No 7.0 EC50 = 111 nM Funct
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
280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1
CHEMBL844 ada1a_bovin Bovine Yes 6.0 EC50 = 1132 nM Funct
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
291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1
CHEMBL260575 ada1a_human Human No 5.9 EC50 = 1150 nM Funct
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
261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1
CHEMBL1437 ada1a_rat Rat Yes 5.9 EC50 = 1174.9 nM Funct
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
169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O
CHEMBL469127 ada1a_human Human No 7.9 EC50 = 12 nM Funct
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
305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1
CHEMBL512062 ada1a_human Human No 7.9 EC50 = 12 nM Funct
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
260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1
CHEMBL13852 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1
CHEMBL117581 ada1a_human Human No 7.9 EC50 = 12.6 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1
CHEMBL420683 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1
CHEMBL71001 ada1a_human Human No 7.9 EC50 = 12.6 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1
CHEMBL13852 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
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
216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1
CHEMBL341747 ada1a_human Human No 7.9 EC50 = 12.6 nM Funct
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
273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1
CHEMBL420683 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
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
253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1
CHEMBL17776 ada1a_human Human No 7.9 EC50 = 12.6 nM Funct
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
284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL13852 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
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.
216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1
CHEMBL329928 ada1a_human Human No 7.9 EC50 = 12.6 nM Funct
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.
247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1
CHEMBL99362 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
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.
246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL13852 ada1a_human Human Yes 7.9 EC50 = 12.6 nM Funct
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
216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1
CHEMBL30596 ada1a_human Human Yes 6.9 EC50 = 120 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2
CHEMBL3956998 ada1a_human Human No 6.9 EC50 = 120.6 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
438 9 1 5 3.4 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1
CHEMBL466296 ada1a_human Human No 6.9 EC50 = 123 nM Funct
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
198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1
CHEMBL116843 ada1a_human Human Yes 6.9 EC50 = 125.9 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1
CHEMBL342324 ada1a_human Human No 6.9 EC50 = 125.9 nM Funct
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
267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1
CHEMBL95245 ada1a_human Human Yes 6.9 EC50 = 125.9 nM Funct
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.
272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1
CHEMBL4080868 ada1a_human Human No 5.9 EC50 = 1250 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
430 10 4 6 2.5 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C4CC4)c3)ccc12
CHEMBL358802 ada1a_human Human Yes 5.9 EC50 = 1258.9 nM Funct
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
254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1
CHEMBL109848 ada1a_rabit Rabbit No 5.9 EC50 = 1288.3 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
255 2 2 2 2.8 CC(=O)Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL257801 ada1a_human Human No 5.9 EC50 = 1340 nM Funct
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
305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1
CHEMBL3400597 ada1a_human Human No 6.9 EC50 = 138.2 nM Bind
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
335 6 0 3 2.9 O=C1CCCN1CCCCN1CCN(c2ccccc2Cl)CC1
CHEMBL3547118 ada1a_human Human No 6.9 EC50 = 138.2 nM Bind
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
335 6 0 3 2.9 O=C1CCCN1CCCCN1CCN(c2ccccc2Cl)CC1
CHEMBL406316 ada1a_human Human No 7.9 EC50 = 14 nM Funct
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
250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2
CHEMBL71001 ada1a_human Human No 7.9 EC50 = 14.1 nM Funct
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
283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1
CHEMBL3986337 ada1a_human Human No 6.9 EC50 = 140.1 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
455 9 1 6 3.3 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cncc3ccccc23)CC1
CHEMBL257977 ada1a_human Human No 6.9 EC50 = 142 nM Funct
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
291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1
CHEMBL466869 ada1a_human Human No 6.8 EC50 = 144 nM Funct
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
228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1
CHEMBL3937911 ada1a_human Human No 6.8 EC50 = 148.2 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cc(Cl)ccc2F)CC1
CHEMBL511211 ada1a_human Human No 7.8 EC50 = 15 nM Funct
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
268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1
CHEMBL154023 ada1a_human Human No 7.8 EC50 = 15.1 nM Funct
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
256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1
CHEMBL116700 ada1a_human Human No 7.8 EC50 = 15.9 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1
CHEMBL97044 ada1a_human Human No 7.8 EC50 = 15.9 nM Funct
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.
258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1
CHEMBL304747 ada1a_rat Rat Yes 5.8 EC50 = 1500 nM Funct
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O
CHEMBL3600395 ada1a_human Human No 5.8 EC50 = 1548 nM Funct
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
430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1
CHEMBL115977 ada1a_human Human No 6.8 EC50 = 158.5 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1
CHEMBL143766 ada1a_human Human No 6.8 EC50 = 158.5 nM Funct
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
273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1
CHEMBL72958 ada1a_human Human Yes 6.8 EC50 = 158.5 nM Funct
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
248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O
CHEMBL74467 ada1a_human Human No 7.8 EC50 = 16.6 nM Funct
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
271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1
CHEMBL108804 ada1a_rabit Rabbit No 7.8 EC50 = 17.0 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
307 3 3 4 2.0 CS(=O)(=O)Nc1c(O)ccc2c1CCCC2c1c[nH]cn1
CHEMBL3968662 ada1a_human Human No 6.8 EC50 = 160.7 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
464 11 1 7 2.8 COc1ccc(S(=O)(=O)NCC2CCN(CCOc3ccccc3OC)CC2)cc1OC
CHEMBL4104183 ada1a_human Human No 6.8 EC50 = 163 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
432 11 4 6 2.7 CCCS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C)n[nH]c3c2)c1
CHEMBL449279 ada1a_human Human Yes 5.8 EC50 = 1650 nM Funct
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
184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2
CHEMBL1215 ada1a_rat Rat Yes 5.8 EC50 = 1659.6 nM Funct
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
167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O
CHEMBL256984 ada1a_human Human No 6.8 EC50 = 167 nM Funct
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
228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1
CHEMBL473425 ada1a_human Human No 6.8 EC50 = 168 nM Funct
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
242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1
CHEMBL2261355 ada1a_rabit Rabbit No 6.8 EC50 = 169.8 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCC[C@H]2c1c[nH]cn1
CHEMBL514333 ada1a_human Human No 7.8 EC50 = 17 nM Funct
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
282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1
CHEMBL117381 ada1a_human Human Yes 7.8 EC50 = 17.4 nM Funct
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
242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1
CHEMBL407308 ada1a_human Human No 6.8 EC50 = 170 nM Funct
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
251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2
CHEMBL286702 ada1a_human Human No 6.8 EC50 = 170 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21
CHEMBL4105097 ada1a_human Human No 5.8 EC50 = 1757 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
432 10 4 6 2.7 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(=O)(=O)C(C)C)c3)ccc12
CHEMBL466012 ada1a_human Human No 7.7 EC50 = 19 nM Funct
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
317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1
CHEMBL505414 ada1a_human Human No 7.7 EC50 = 19 nM Funct
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
280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1
CHEMBL449284 ada1a_human Human No 7.7 EC50 = 19 nM Funct
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
218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1
CHEMBL117381 ada1a_human Human Yes 7.7 EC50 = 20.0 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1
CHEMBL17492 ada1a_human Human No 7.7 EC50 = 20.0 nM Funct
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
254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1
CHEMBL762 ada1a_human Human Yes 7.7 EC50 = 20.0 nM Funct
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.
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL100198 ada1a_human Human No 7.7 EC50 = 20.0 nM Funct
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.
246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL100383 ada1a_human Human No 7.7 EC50 = 20.0 nM Funct
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.
289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1
CHEMBL320419 ada1a_human Human No 7.7 EC50 = 20.0 nM Funct
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.
274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL762 ada1a_human Human Yes 7.7 EC50 = 20.0 nM Funct
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
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL322492 ada1a_rabit Rabbit No 4.7 EC50 = 19054.6 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
305 3 2 3 2.6 CS(=O)(=O)Nc1cccc2c1CCCCC2c1c[nH]cn1
CHEMBL3948333 ada1a_human Human No 6.7 EC50 = 191.6 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
450 10 1 7 2.5 COc1ccc(S(=O)(=O)NC2CCN(CCOc3ccccc3OC)CC2)cc1OC
CHEMBL74071 ada1a_human Human No 5.7 EC50 = 1949.8 nM Funct
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
281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL448510 ada1a_human Human No 6.7 EC50 = 195 nM Funct
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
295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1
CHEMBL18436 ada1a_human Human No 6.7 EC50 = 199.5 nM Funct
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
298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL448802 ada1a_human Human No 8.7 EC50 = 2 nM Funct
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
251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1
CHEMBL346380 ada1a_human Human No 8.7 EC50 = 2.2 nM Funct
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
257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1
CHEMBL72768 ada1a_human Human No 8.6 EC50 = 2.3 nM Funct
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
239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1
CHEMBL142871 ada1a_human Human Yes 8.6 EC50 = 2.5 nM Funct
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
259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1
CHEMBL143973 ada1a_human Human Yes 8.6 EC50 = 2.5 nM Funct
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
254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1
CHEMBL275902 ada1a_human Human No 8.6 EC50 = 2.5 nM Funct
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
268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1
CHEMBL95523 ada1a_human Human No 8.6 EC50 = 2.5 nM Funct
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.
232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL152725 ada1a_human Human No 8.6 EC50 = 2.7 nM Funct
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
255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1
CHEMBL70634 ada1a_human Human No 8.6 EC50 = 2.8 nM Funct
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
287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1
CHEMBL762 ada1a_human Human Yes 7.7 EC50 = 20.4 nM Funct
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
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL356195 ada1a_human Human No 7.7 EC50 = 20.9 nM Funct
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
246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1
CHEMBL33405 ada1a_human Human No 6.7 EC50 = 200 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21
CHEMBL260576 ada1a_human Human No 5.7 EC50 = 2060 nM Funct
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
261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1
CHEMBL109783 ada1a_human Human Yes 7.7 EC50 = 21.9 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1
CHEMBL257977 ada1a_human Human No 5.7 EC50 = 2150 nM Funct
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
291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1
CHEMBL1437 ada1a_human Human Yes 5.7 EC50 = 2187.8 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O
CHEMBL3601200 ada1a_human Human No 6.7 EC50 = 219 nM Funct
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
404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL3601200 ada1a_human Human No 6.7 EC50 = 219 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL467688 ada1a_human Human No 7.7 EC50 = 22 nM Funct
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
214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1
CHEMBL257976 ada1a_human Human No 5.7 EC50 = 2200 nM Funct
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
241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1
CHEMBL419448 ada1a_human Human No 7.6 EC50 = 24.0 nM Funct
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
271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1
CHEMBL257977 ada1a_human Human No 6.6 EC50 = 234 nM Funct
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
291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1
CHEMBL466296 ada1a_human Human No 6.6 EC50 = 234 nM Funct
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
198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1
CHEMBL70973 ada1a_human Human No 6.6 EC50 = 239.9 nM Funct
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
267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL154170 ada1a_human Human No 7.6 EC50 = 24.6 nM Funct
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
266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1
CHEMBL133451 ada1a_human Human No 4.6 EC50 = 24547.1 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1
CHEMBL257978 ada1a_human Human Yes 7.6 EC50 = 25 nM Funct
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
317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1
CHEMBL1191956 ada1a_human Human Yes 7.6 EC50 = 25 nM Bind
Effective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear arteryEffective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear artery
244 5 3 4 0.5 CNCCc1ccc(O)c(NS(C)(=O)=O)c1
CHEMBL543126 ada1a_human Human Yes 7.6 EC50 = 25 nM Bind
Effective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear arteryEffective concentration (EC50) against alpha-1-adrenoceptor in the isolated rabbit ear artery
244 5 3 4 0.5 CNCCc1ccc(O)c(NS(C)(=O)=O)c1
CHEMBL142958 ada1a_human Human No 7.6 EC50 = 25.1 nM Funct
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
272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1
CHEMBL344957 ada1a_human Human No 7.6 EC50 = 25.1 nM Funct
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
273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1
CHEMBL417999 ada1a_human Human No 7.6 EC50 = 25.1 nM Funct
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
269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1
CHEMBL275386 ada1a_human Human No 6.6 EC50 = 251.2 nM Funct
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
283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1
CHEMBL111734 ada1a_rabit Rabbit Yes 5.6 EC50 = 2511.9 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
279 5 2 3 2.1 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1C
CHEMBL3601201 ada1a_human Human No 6.6 EC50 = 252 nM Funct
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
420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL1079 ada1a_bovin Bovine Yes 6.6 EC50 = 264 nM Funct
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
253 1 2 6 1.7 Clc1ccc2nsnc2c1NC1=NCCN1
CHEMBL466635 ada1a_human Human No 7.6 EC50 = 27 nM Funct
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
268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1
CHEMBL481322 ada1a_human Human Yes 7.6 EC50 = 27 nM Funct
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
262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1
CHEMBL323402 ada1a_rabit Rabbit Yes 6.6 EC50 = 275.4 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
213 1 2 2 2.5 Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL465599 ada1a_human Human No 6.6 EC50 = 276 nM Funct
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
232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1
CHEMBL3601202 ada1a_human Human No 6.6 EC50 = 277 nM Funct
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
434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL406348 ada1a_human Human No 6.6 EC50 = 278 nM Funct
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
264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1
CHEMBL321644 ada1a_rabit Rabbit No 5.6 EC50 = 2818.4 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
359 4 2 3 3.2 O=S(=O)(CC(F)(F)F)Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL762 ada1a_rat Rat Yes 6.5 EC50 = 288.4 nM Funct
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
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL1215 ada1a_human Human Yes 5.5 EC50 = 2951.2 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O
CHEMBL466634 ada1a_human Human No 8.5 EC50 = 3 nM Funct
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
269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1
CHEMBL468710 ada1a_human Human No 8.5 EC50 = 3 nM Funct
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
267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1
CHEMBL509350 ada1a_human Human No 8.5 EC50 = 3 nM Funct
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
268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1
CHEMBL260720 ada1a_human Human No 8.5 EC50 = 3 nM Funct
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
264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1
CHEMBL13789 ada1a_human Human No 8.5 EC50 = 3.2 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1
CHEMBL13789 ada1a_human Human No 8.5 EC50 = 3.2 nM Funct
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
252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1
CHEMBL143562 ada1a_human Human Yes 8.5 EC50 = 3.2 nM Funct
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
256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1
CHEMBL17856 ada1a_human Human No 8.5 EC50 = 3.2 nM Funct
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
255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1
CHEMBL319553 ada1a_human Human No 8.5 EC50 = 3.2 nM Funct
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.
261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1
CHEMBL156950 ada1a_human Human No 8.5 EC50 = 3.3 nM Funct
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
260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1
CHEMBL1190038 ada1a_human Human No 8.5 EC50 = 3.4 nM Funct
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
235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1
CHEMBL540035 ada1a_human Human No 8.5 EC50 = 3.4 nM Funct
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
235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1
CHEMBL325745 ada1a_human Human No 8.4 EC50 = 4.0 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1
CHEMBL66433 ada1a_rat Rat No 5.5 EC50 = 3000 nM Funct
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12
CHEMBL284307 ada1a_human Human Yes 4.5 EC50 = 30000 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2
CHEMBL286226 ada1a_human Human No 4.5 EC50 = 30000 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1
CHEMBL286609 ada1a_human Human No 4.5 EC50 = 30000 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1
CHEMBL133451 ada1a_rat Rat No 4.5 EC50 = 30903.0 nM Funct
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
309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1
CHEMBL481322 ada1a_human Human Yes 7.5 EC50 = 31 nM Funct
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
262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1
CHEMBL481322 ada1a_human Human Yes 7.5 EC50 = 31 nM Funct
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
262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1
CHEMBL421011 ada1a_human Human No 7.5 EC50 = 31.6 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL421011 ada1a_human Human No 7.5 EC50 = 31.6 nM Funct
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
274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL421011 ada1a_human Human No 7.5 EC50 = 31.6 nM Funct
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.
274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL466296 ada1a_human Human No 6.5 EC50 = 315 nM Funct
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
198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1
CHEMBL72958 ada1a_human Human Yes 6.5 EC50 = 316.2 nM Funct
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
248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O
CHEMBL277361 ada1a_human Human No 6.5 EC50 = 316.2 nM Funct
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
323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1
CHEMBL402388 ada1a_human Human Yes 7.5 EC50 = 32 nM Funct
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
214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1
CHEMBL404566 ada1a_human Human No 7.5 EC50 = 32 nM Funct
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
291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1
CHEMBL482148 ada1a_human Human No 7.5 EC50 = 32 nM Funct
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
264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2
CHEMBL402003 ada1a_human Human No 6.5 EC50 = 322 nM Funct
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
284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1
CHEMBL152154 ada1a_human Human No 6.5 EC50 = 323.6 nM Funct
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
256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1
CHEMBL3400594 ada1a_human Human No 6.5 EC50 = 329.1 nM Bind
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
427 8 0 3 4.1 O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL3547015 ada1a_human Human No 6.5 EC50 = 329.1 nM Bind
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
427 8 0 3 4.1 O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL501404 ada1a_human Human No 7.5 EC50 = 33 nM Funct
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
269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1
CHEMBL3601310 ada1a_human Human No 7.5 EC50 = 33 nM Funct
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
420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1
CHEMBL255938 ada1a_human Human No 7.5 EC50 = 33 nM Funct
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
291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1
CHEMBL43711 ada1a_human Human Yes 5.5 EC50 = 3300 nM Funct
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
201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F
CHEMBL3894175 ada1a_human Human No 7.5 EC50 = 34.1 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
483 10 1 6 4.1 CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc3cccnc23)CC1
CHEMBL285082 ada1a_human Human No 6.5 EC50 = 340 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N
CHEMBL762 ada1a_human Human Yes 6.5 EC50 = 346.7 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL467495 ada1a_human Human No 5.5 EC50 = 3460 nM Funct
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
218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1
CHEMBL351543 ada1a_human Human No 7.4 EC50 = 36.3 nM Funct
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
271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1
CHEMBL473424 ada1a_human Human No 7.4 EC50 = 37 nM Funct
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
228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1
CHEMBL511576 ada1a_human Human No 6.4 EC50 = 371 nM Funct
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
227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1
CHEMBL778 ada1a_bovin Bovine Yes 6.4 EC50 = 376 nM Funct
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
200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C
CHEMBL347268 ada1a_human Human No 7.4 EC50 = 38.9 nM Funct
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
256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1
CHEMBL258007 ada1a_human Human Yes 6.4 EC50 = 385 nM Funct
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
198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1
CHEMBL142967 ada1a_human Human No 7.4 EC50 = 39.8 nM Funct
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
256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1
CHEMBL329272 ada1a_human Human No 7.4 EC50 = 39.8 nM Funct
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.
287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1
CHEMBL63976 ada1a_rat Rat Yes 5.4 EC50 = 3900 nM Funct
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12
CHEMBL273312 ada1a_human Human No 6.4 EC50 = 398.1 nM Funct
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
255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1
CHEMBL95333 ada1a_human Human No 6.4 EC50 = 398.1 nM Funct
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.
286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1
CHEMBL513871 ada1a_human Human No 8.4 EC50 = 4 nM Funct
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
353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1
CHEMBL434074 ada1a_human Human No 8.4 EC50 = 4.5 nM Funct
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
272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1
CHEMBL117248 ada1a_human Human Yes 8.3 EC50 = 4.6 nM Funct
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
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL540542 ada1a_human Human Yes 8.3 EC50 = 4.6 nM Funct
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
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL349082 ada1a_human Human No 8.3 EC50 = 4.6 nM Funct
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
253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1
CHEMBL679 ada1a_human Human Yes 6.4 EC50 = 400 nM Funct
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
183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O
CHEMBL74114 ada1a_human Human No 7.4 EC50 = 41.7 nM Funct
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
271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1
CHEMBL511411 ada1a_human Human No 7.4 EC50 = 42 nM Funct
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
202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1
CHEMBL156893 ada1a_human Human No 7.4 EC50 = 42.7 nM Funct
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
268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1
CHEMBL260116 ada1a_human Human No 6.4 EC50 = 426 nM Funct
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
267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2
CHEMBL256982 ada1a_human Human No 7.4 EC50 = 43 nM Funct
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
325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1
CHEMBL256982 ada1a_human Human No 7.4 EC50 = 43 nM Funct
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
325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1
CHEMBL256982 ada1a_human Human No 7.4 EC50 = 43 nM Funct
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
325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1
CHEMBL70326 ada1a_human Human No 6.4 EC50 = 436.5 nM Funct
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
271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1
CHEMBL207277 ada1a_rat Rat No 5.4 EC50 = 4400 nM Funct
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
CHEMBL111554 ada1a_rabit Rabbit Yes 6.4 EC50 = 446.7 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL154346 ada1a_human Human No 7.3 EC50 = 45.7 nM Funct
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
242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1
CHEMBL255937 ada1a_human Human No 6.4 EC50 = 451 nM Funct
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
248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1
CHEMBL258178 ada1a_human Human Yes 6.3 EC50 = 473 nM Funct
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
184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1
CHEMBL258178 ada1a_human Human Yes 6.3 EC50 = 473 nM Funct
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
184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1
CHEMBL466876 ada1a_human Human No 7.3 EC50 = 48 nM Funct
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
242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1
CHEMBL1191324 ada1a_human Human No 6.3 EC50 = 489.8 nM Funct
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
237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1
CHEMBL542402 ada1a_human Human No 6.3 EC50 = 489.8 nM Funct
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
237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1
CHEMBL448908 ada1a_human Human No 8.3 EC50 = 5 nM Funct
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
250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1
CHEMBL510023 ada1a_human Human No 8.3 EC50 = 5 nM Funct
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
268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1
CHEMBL117248 ada1a_human Human Yes 8.3 EC50 = 5.0 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL540542 ada1a_human Human Yes 8.3 EC50 = 5.0 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL142387 ada1a_human Human No 8.3 EC50 = 5.0 nM Funct
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
259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1
CHEMBL344551 ada1a_human Human No 8.3 EC50 = 5.0 nM Funct
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
242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1
CHEMBL1194763 ada1a_human Human No 8.3 EC50 = 5.0 nM Funct
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
249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1
CHEMBL553276 ada1a_human Human No 8.3 EC50 = 5.0 nM Funct
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
249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1
CHEMBL336161 ada1a_rat Rat Yes 8.3 EC50 = 5.2 nM Funct
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
309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1
CHEMBL336161 ada1a_human Human Yes 8.3 EC50 = 5.6 nM Funct
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1
CHEMBL109783 ada1a_rat Rat Yes 8.2 EC50 = 5.8 nM Funct
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
309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1
CHEMBL117094 ada1a_human Human Yes 7.3 EC50 = 50.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL544290 ada1a_human Human Yes 7.3 EC50 = 50.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL325648 ada1a_human Human Yes 7.3 EC50 = 50.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1
CHEMBL326067 ada1a_human Human No 7.3 EC50 = 50.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1
CHEMBL441412 ada1a_human Human No 7.3 EC50 = 50.1 nM Funct
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
268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C
CHEMBL450018 ada1a_human Human No 7.3 EC50 = 50.1 nM Funct
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.
260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL98016 ada1a_human Human No 7.3 EC50 = 50.1 nM Funct
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.
260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1
CHEMBL432192 ada1a_human Human No 6.3 EC50 = 501.2 nM Funct
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.
274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1
CHEMBL95398 ada1a_human Human No 6.3 EC50 = 501.2 nM Funct
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.
275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1
CHEMBL466046 ada1a_human Human No 7.3 EC50 = 51 nM Funct
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
209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1
CHEMBL467916 ada1a_human Human No 7.3 EC50 = 51 nM Funct
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
209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1
CHEMBL611 ada1a_human Human Yes 7.3 EC50 = 51 nM Bind
Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assayAntagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1
CHEMBL351542 ada1a_human Human No 7.3 EC50 = 51.3 nM Funct
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
232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1
CHEMBL611 ada1a_human Human Yes 7.3 EC50 = 51.9 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1
CHEMBL70563 ada1a_human Human No 6.3 EC50 = 512.9 nM Funct
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
287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1
CHEMBL503269 ada1a_human Human No 6.3 EC50 = 514 nM Funct
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
232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1
CHEMBL256983 ada1a_human Human No 7.3 EC50 = 52 nM Funct
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
250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2
CHEMBL346465 ada1a_human Human No 7.3 EC50 = 52.5 nM Funct
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
260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1
CHEMBL284486 ada1a_human Human No 5.3 EC50 = 5300 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2
CHEMBL111584 ada1a_rabit Rabbit No 5.3 EC50 = 5495.4 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
305 3 1 4 2.3 Cn1cnc(C2CCCc3c(NS(C)(=O)=O)cccc32)c1
CHEMBL1215 ada1a_human Human Yes 7.3 EC50 = 55 nM Bind
Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assayAgonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay
167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O
CHEMBL1215 ada1a_human Human Yes 7.3 EC50 = 56.0 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O
CHEMBL117094 ada1a_human Human Yes 7.3 EC50 = 56.2 nM Funct
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
253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL544290 ada1a_human Human Yes 7.3 EC50 = 56.2 nM Funct
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
253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1
CHEMBL325897 ada1a_rabit Rabbit No 5.3 EC50 = 5623.4 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
317 4 2 3 2.8 O=S(=O)(Nc1cccc2c1CCCC2c1c[nH]cn1)C1CC1
CHEMBL507755 ada1a_human Human No 6.2 EC50 = 578 nM Funct
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
214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1
CHEMBL481321 ada1a_human Human No 7.2 EC50 = 59 nM Funct
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
246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1
CHEMBL114669 ada1a_human Human No 8.2 EC50 = 6.3 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1
CHEMBL327005 ada1a_human Human No 8.2 EC50 = 6.3 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1
CHEMBL17151 ada1a_human Human No 8.2 EC50 = 6.3 nM Funct
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
284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL18256 ada1a_human Human No 8.2 EC50 = 6.3 nM Funct
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
255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1
CHEMBL154298 ada1a_human Human No 8.2 EC50 = 6.8 nM Funct
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
252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1
CHEMBL326702 ada1a_rabit Rabbit Yes 7.2 EC50 = 60 nM Funct
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1
CHEMBL326702 ada1a_human Human Yes 6.2 EC50 = 600 nM Bind
Effective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1A adrenergic receptor
265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1
CHEMBL326702 ada1a_rabit Rabbit Yes 6.2 EC50 = 602.6 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1
CHEMBL3601203 ada1a_human Human No 7.2 EC50 = 61 nM Funct
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
424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1
CHEMBL467259 ada1a_human Human No 7.2 EC50 = 62 nM Funct
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
280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1
CHEMBL473043 ada1a_human Human No 7.2 EC50 = 62 nM Funct
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
242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1
CHEMBL502078 ada1a_human Human No 7.2 EC50 = 62 nM Funct
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
246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1
CHEMBL114054 ada1a_human Human No 7.2 EC50 = 63.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1
CHEMBL117482 ada1a_human Human No 7.2 EC50 = 63.1 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1
CHEMBL17221 ada1a_human Human No 7.2 EC50 = 63.1 nM Funct
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
269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1
CHEMBL761 ada1a_human Human Yes 7.2 EC50 = 63.1 nM Funct
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.
210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2
CHEMBL761 ada1a_human Human Yes 7.2 EC50 = 63.1 nM Funct
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
210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2
CHEMBL111496 ada1a_rabit Rabbit Yes 6.2 EC50 = 631.0 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
305 4 2 3 2.6 CCS(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL480272 ada1a_human Human No 6.2 EC50 = 658 nM Funct
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
246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1
CHEMBL111771 ada1a_rabit Rabbit No 7.2 EC50 = 66.1 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1c[nH]cn1
CHEMBL347920 ada1a_human Human No 6.2 EC50 = 660.7 nM Funct
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
257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1
CHEMBL350906 ada1a_human Human No 6.2 EC50 = 676.1 nM Funct
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
320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1
CHEMBL111537 ada1a_rabit Rabbit No 5.2 EC50 = 6760.8 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
319 4 2 3 3.0 CC(C)S(=O)(=O)Nc1cccc2c1CCCC2c1c[nH]cn1
CHEMBL306792 ada1a_human Human No 8.1 EC50 = 7.8 nM Funct
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
239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1
CHEMBL70692 ada1a_human Human No 8.1 EC50 = 7.8 nM Funct
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
239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1
CHEMBL318544 ada1a_human Human No 8.1 EC50 = 7.9 nM Funct
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL337862 ada1a_human Human No 8.1 EC50 = 7.9 nM Funct
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
251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1
CHEMBL318544 ada1a_human Human No 8.1 EC50 = 7.9 nM Funct
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.
260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL98243 ada1a_human Human No 8.1 EC50 = 7.9 nM Funct
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.
275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1
CHEMBL257800 ada1a_human Human No 7.2 EC50 = 70 nM Funct
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
277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1
CHEMBL465963 ada1a_human Human No 7.2 EC50 = 70 nM Funct
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
184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1
CHEMBL1076 ada1a_rabit Rabbit Yes 5.2 EC50 = 7079.5 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1
CHEMBL1076 ada1a_human Human Yes 5.2 EC50 = 7100 nM Bind
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
197 4 2 4 0.7 COc1ccc(OC)c(C(O)CN)c1
CHEMBL287587 ada1a_human Human Yes 4.2 EC50 = 71000 nM Funct
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
187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F
CHEMBL524 ada1a_human Human Yes 6.1 EC50 = 720 nM Funct
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC
CHEMBL466914 ada1a_human Human Yes 6.1 EC50 = 721 nM Funct
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
198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1
CHEMBL358685 ada1a_human Human No 6.1 EC50 = 724.4 nM Funct
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
257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1
CHEMBL465963 ada1a_human Human No 7.1 EC50 = 73 nM Funct
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
184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1
CHEMBL466876 ada1a_human Human No 7.1 EC50 = 76 nM Funct
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
242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1
CHEMBL257799 ada1a_human Human No 7.1 EC50 = 78 nM Funct
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
284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1
CHEMBL257799 ada1a_human Human No 7.1 EC50 = 78 nM Funct
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
284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1
CHEMBL17764 ada1a_human Human No 7.1 EC50 = 79.4 nM Funct
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
324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1
CHEMBL95565 ada1a_human Human No 7.1 EC50 = 79.4 nM Funct
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.
274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL17657 ada1a_human Human No 6.1 EC50 = 794.3 nM Funct
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
256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1
CHEMBL42359 ada1a_human Human Yes 6.1 EC50 = 800 nM Funct
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
201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F
CHEMBL512289 ada1a_human Human No 7.1 EC50 = 81 nM Funct
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
261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1
CHEMBL67457 ada1a_rat Rat Yes 6.1 EC50 = 810 nM Funct
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
284 2 0 3 3.2 Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
CHEMBL3601308 ada1a_human Human No 6.1 EC50 = 812 nM Funct
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
458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1
CHEMBL511577 ada1a_human Human No 7.1 EC50 = 82 nM Funct
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
228 3 0 3 2.4 COCc1ccccc1C1Cc2nccn2C1
CHEMBL465963 ada1a_human Human No 7.1 EC50 = 83 nM Funct
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
184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1
CHEMBL499180 ada1a_human Human No 7.1 EC50 = 84 nM Funct
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
276 3 1 3 2.0 CS(=O)(=O)Cc1cccc2c1CCC2c1ncc[nH]1
CHEMBL3895815 ada1a_human Human No 7.1 EC50 = 84.2 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
456 9 1 5 3.6 COc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2F)CC1
CHEMBL3601204 ada1a_human Human No 6.1 EC50 = 857 nM Funct
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
418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL3601204 ada1a_human Human No 6.1 EC50 = 857 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12
CHEMBL439822 ada1a_human Human No 7.1 EC50 = 87.1 nM Funct
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
260 6 2 5 1.9 CC/C(=N/OC)c1ccccc1NCC1=NCCN1
CHEMBL510613 ada1a_human Human No 6.1 EC50 = 879 nM Funct
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
289 3 1 2 2.9 FC1(F)CN(Cc2cccc3c2CCC3c2ncc[nH]2)C1
CHEMBL134 ada1a_bovin Bovine Yes 7.1 EC50 = 89 nM Funct
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
229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl
CHEMBL1215 ada1a_bovin Bovine Yes 8.1 EC50 = 9 nM Funct
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
167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O
CHEMBL508084 ada1a_human Human No 8.1 EC50 = 9 nM Funct
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
264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1
CHEMBL326702 ada1a_human Human Yes 8.1 EC50 = 9 nM Funct
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
265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1
CHEMBL474796 ada1a_human Human No 8.1 EC50 = 9 nM Funct
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
300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1
CHEMBL1437 ada1a_human Human Yes 8.0 EC50 = 9.1 nM Funct
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
169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O
CHEMBL1437 ada1a_human Human Yes 8.0 EC50 = 9.1 nM Funct
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assayAgonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O
CHEMBL109783 ada1a_human Human Yes 8.0 EC50 = 9.3 nM Bind
Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptorEffective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor
309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1
CHEMBL109783 ada1a_rabit Rabbit Yes 8.0 EC50 = 9.3 nM Bind
Agonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethraAgonist activity at alpha1A adrenoreceptor in Oryctolagus cuniculus (rabbit) urethra
309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1
CHEMBL520117 ada1a_human Human No 7.1 EC50 = 90 nM Funct
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
265 3 1 4 2.1 c1cc(Cn2ccnn2)c2c(c1)C(c1ncc[nH]1)CC2
CHEMBL448147 ada1a_human Human No 7.0 EC50 = 92 nM Funct
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
251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1
CHEMBL501920 ada1a_human Human No 6.0 EC50 = 939 nM Funct
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
214 2 0 3 2.2 COc1ccc(C2Cc3nccn3C2)cc1
CHEMBL3939560 ada1a_human Human No 7.0 EC50 = 99.7 nM Bind
Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assayIntrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
441 8 1 6 3.1 COc1ccccc1OCCN1CCC(NS(=O)(=O)c2cncc3ccccc23)CC1
CHEMBL1628227 ada1a_rat Rat Yes 11.0 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21
CHEMBL629 ada1a_rat Rat Yes 10.7 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C
CHEMBL1200710 ada1a_rat Rat Yes 10.4 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL415 ada1a_rat Rat Yes 10.4 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL1201156 ada1a_rat Rat Yes 10.4 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL445 ada1a_rat Rat Yes 10.4 IC50 = 0.0 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL6437 ada1a_rat Rat Yes 10.2 IC50 = 0.1 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1
CHEMBL2 ada1a_rat Rat Yes 9.7 IC50 = 0.2 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1
CHEMBL1696 ada1a_rat Rat Yes 9.6 IC50 = 0.3 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21
CHEMBL72 ada1a_rat Rat Yes 9.6 IC50 = 0.3 nM Bind
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorCompound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21
CHEMBL2 ada1a_rat Rat Yes 9.6 IC50 = 0.3 nM Bind
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1
CHEMBL2153423 ada1a_rat Rat No 9.6 IC50 = 0.3 nM Bind
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1
CHEMBL2220978 ada1a_rat Rat No 9.6 IC50 = 0.3 nM Bind
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counterDisplacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter
340 5 0 5 2.8 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCO3)CC1
CHEMBL3810110 ada1a_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
443 12 3 6 2.9 COc1ccc(F)cc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL836 ada1a_human Human Yes 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C
CHEMBL304438 ada1a_bovin Bovine No 9.3 IC50 = 0.5 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1
CHEMBL3892879 ada1a_rat Rat No 9.3 IC50 = 0.5 nM Bind
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4
CHEMBL60885 ada1a_bovin Bovine No 9.2 IC50 = 0.6 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1
CHEMBL3582270 ada1a_human Human No 9.2 IC50 = 0.6 nM Bind
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
599 8 1 13 2.7 CCN(CC)c1ccc2cc(-n3cc(C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1
CHEMBL2 ada1a_rat Rat Yes 9.2 IC50 = 0.7 nM Bind
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1
CHEMBL707 ada1a_rat Rat Yes 9.1 IC50 = 0.7 nM Bind
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2
CHEMBL24778 ada1a_rat Rat Yes 9.1 IC50 = 0.8 nM Bind
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N
CHEMBL64878 ada1a_bovin Bovine No 9.1 IC50 = 0.8 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1
CHEMBL85 ada1a_rat Rat Yes 9.0 IC50 = 1.0 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL292935 ada1a_bovin Bovine No 9.0 IC50 = 1 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1
CHEMBL25554 ada1a_human Human Yes 9.0 IC50 = 1 nM Funct
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC
CHEMBL25554 ada1a_human Human Yes 9.0 IC50 = 1 nM Funct
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC
CHEMBL25098 ada1a_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
539 9 1 6 5.5 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OC(C)C)CC3)cccc2c1=O
CHEMBL278518 ada1a_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
529 7 1 5 5.7 Cc1ccc(Cl)cc1N1CCN(CCCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1
CHEMBL597 ada1a_human Human Yes 9.0 IC50 = 1.1 nM Bind
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1
CHEMBL3810145 ada1a_human Human No 8.9 IC50 = 1.3 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
527 13 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1cc(Cl)ccc1OCC(F)(F)F
CHEMBL27341 ada1a_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
496 8 0 6 5.6 COc1ccccc1N1CCN(CCCC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1
CHEMBL707 ada1a_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2
CHEMBL1255837 ada1a_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL601773 ada1a_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O
CHEMBL1108 ada1a_rat Rat Yes 8.8 IC50 = 1.7 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1
CHEMBL11 ada1a_rat Rat Yes 8.8 IC50 = 1.7 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C
CHEMBL24778 ada1a_human Human Yes 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N
CHEMBL24778 ada1a_human Human Yes 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N
CHEMBL3808572 ada1a_human Human Yes 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
493 13 3 6 3.7 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCC(F)(F)F
CHEMBL3809248 ada1a_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
439 13 3 6 3.1 CCOc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL3809490 ada1a_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1
CHEMBL293923 ada1a_bovin Bovine Yes 8.0 IC50 = 10 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1
CHEMBL85 ada1a_human Human Yes 8.0 IC50 = 10 nM Bind
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL85 ada1a_human Human Yes 8.0 IC50 = 10 nM Funct
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL24629 ada1a_rat Rat No 8.0 IC50 = 10 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
498 9 0 6 5.8 COc1ccccc1N1CCN(CCCCOc2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1
CHEMBL85 ada1a_human Human Yes 8.0 IC50 = 10.9 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL85 ada1a_human Human Yes 8.0 IC50 = 10.9 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL85 ada1a_human Human Yes 8.0 IC50 = 10.9 nM Funct
Antagonist activity at alpha-1a adrenergic receptor (unknown origin)Antagonist activity at alpha-1a adrenergic receptor (unknown origin)
410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2
CHEMBL1203299 ada1a_bovin Bovine No 7.0 IC50 = 100 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
414 5 1 5 3.1 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccc3)CC1)O2
CHEMBL128451 ada1a_bovin Bovine No 7.0 IC50 = 100 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
414 5 1 5 3.1 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccc3)CC1)O2
CHEMBL113830 ada1a_human Human Yes 7.0 IC50 = 100 nM Bind
Inhibition of Alpha-1 adrenergic receptorInhibition of Alpha-1 adrenergic receptor
325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1
CHEMBL420644 ada1a_rat Rat No 7.0 IC50 = 100 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
281 4 1 2 3.7 CN(C)CC(c1ccc(Cl)cc1)C1(O)CCCCC1
CHEMBL51561 ada1a_bovin Bovine No 6.0 IC50 = 1000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1
CHEMBL56990 ada1a_bovin Bovine No 6.0 IC50 = 1000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1
CHEMBL1203297 ada1a_bovin Bovine No 6.0 IC50 = 1000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
439 5 1 6 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc(C#N)cc3)CC1)O2
CHEMBL130410 ada1a_bovin Bovine No 6.0 IC50 = 1000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
439 5 1 6 3.0 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc(C#N)cc3)CC1)O2
CHEMBL143617 ada1a_rat Rat Yes 6.0 IC50 = 1000 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
432 5 1 3 4.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1=CCN(CCN2CCNC2=O)CC1
CHEMBL511747 ada1a_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O
CHEMBL1178987 ada1a_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL52785 ada1a_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2
CHEMBL27763 ada1a_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1
CHEMBL284912 ada1a_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1
CHEMBL508712 ada1a_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12
CHEMBL27995 ada1a_bovin Bovine Yes 4.0 IC50 = 100000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1
CHEMBL280608 ada1a_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL51888 ada1a_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL97044 ada1a_human Human No 6.0 IC50 = 1047.1 nM Bind
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1
CHEMBL1628227 ada1a_rat Rat Yes 7.0 IC50 = 107 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21
CHEMBL117248 ada1a_human Human Yes 7.0 IC50 = 107.2 nM Bind
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL540542 ada1a_human Human Yes 7.0 IC50 = 107.2 nM Bind
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1
CHEMBL4225239 ada1a_human Human No 6.0 IC50 = 1073.9 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1
CHEMBL4300633 ada1a_human Human No 6.0 IC50 = 1073.9 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1
CHEMBL30008 ada1a_rat Rat Yes 6.0 IC50 = 1088 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL539027 ada1a_rat Rat Yes 6.0 IC50 = 1088 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL552659 ada1a_rat Rat Yes 6.0 IC50 = 1088 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL637 ada1a_rat Rat Yes 7.0 IC50 = 109 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1
CHEMBL4210030 ada1a_human Human No 8.0 IC50 = 11 nM Funct
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1
CHEMBL1403281 ada1a_rat Rat Yes 8.0 IC50 = 11 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C
CHEMBL597 ada1a_rat Rat Yes 8.0 IC50 = 11 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1
CHEMBL1385840 ada1a_rat Rat Yes 8.0 IC50 = 11 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12
CHEMBL422130 ada1a_rat Rat Yes 8.0 IC50 = 11 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
440 5 1 3 4.8 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3ccc(Cl)cc32)CC1
CHEMBL332913 ada1a_rat Rat No 7.0 IC50 = 110 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
374 5 0 4 4.1 Fc1ccc(-n2cc(OCCN3CCOCC3)c3cc(Cl)ccc32)cc1
CHEMBL926 ada1a_rat Rat Yes 7.0 IC50 = 110 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O
CHEMBL488251 ada1a_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL165796 ada1a_human Human No 7.0 IC50 = 112.2 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
373 3 0 5 3.7 Cc1ccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1
CHEMBL162490 ada1a_human Human No 6.9 IC50 = 114.8 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
389 4 0 6 3.4 COc1cccn2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc12
CHEMBL420683 ada1a_human Human Yes 6.9 IC50 = 114.8 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1
CHEMBL467668 ada1a_human Human No 5.9 IC50 = 1160 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1
CHEMBL621 ada1a_rat Rat Yes 6.9 IC50 = 117 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2
CHEMBL421239 ada1a_rat Rat No 7.9 IC50 = 12 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
444 9 1 4 4.1 CCN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O
CHEMBL3892879 ada1a_human Human No 7.9 IC50 = 12.8 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4
CHEMBL3805518 ada1a_human Human No 6.9 IC50 = 120 nM Bind
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F
CHEMBL1729 ada1a_rat Rat Yes 6.9 IC50 = 120 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL560739 ada1a_rat Rat Yes 6.9 IC50 = 120 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N
CHEMBL3739900 ada1a_human Human No 5.9 IC50 = 1200 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
439 7 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(Cc3ccccc3)CC2)cc1
CHEMBL8412 ada1a_bovin Bovine Yes 5.9 IC50 = 1200 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL361506 ada1a_rat Rat Yes 5.9 IC50 = 1212 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1
CHEMBL55 ada1a_rat Rat Yes 5.9 IC50 = 1212 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1
CHEMBL4227241 ada1a_human Human No 5.9 IC50 = 1212.5 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1
CHEMBL4300995 ada1a_human Human No 5.9 IC50 = 1212.5 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1
CHEMBL15245 ada1a_rat Rat Yes 5.9 IC50 = 1235 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1
CHEMBL4104261 ada1a_human Human No 6.9 IC50 = 124 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F
CHEMBL4284346 ada1a_human Human No 6.9 IC50 = 124 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL3957222 ada1a_human Human No 6.9 IC50 = 124.7 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
440 5 1 4 5.4 COc1ccc2[nH]c3c(c2c1)CC1c2cc(OCc4ccccc4)c(OC)cc2CCN1C3
CHEMBL3932187 ada1a_human Human No 6.9 IC50 = 125 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4
CHEMBL100774 ada1a_rat Rat No 6.9 IC50 = 126 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
263 5 1 3 2.6 COc1ccc(C(CN(C)C)C2(O)CCCC2)cc1
CHEMBL3740874 ada1a_human Human No 6.9 IC50 = 128 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
468 6 0 5 3.9 N#Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)c(F)c1
CHEMBL344294 ada1a_human Human No 5.9 IC50 = 1288.3 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
267 4 1 4 2.4 Cc1ccnc(-c2ccccc2OCC2=NCCN2)c1
CHEMBL454246 ada1a_human Human No 7.9 IC50 = 13 nM Funct
Inhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C
CHEMBL123640 ada1a_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12
CHEMBL101899 ada1a_rat Rat Yes 6.9 IC50 = 130 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
281 4 1 2 3.7 CN(C)CC(c1cccc(Cl)c1)C1(O)CCCCC1
CHEMBL1696 ada1a_rat Rat Yes 6.9 IC50 = 130 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21
CHEMBL72 ada1a_rat Rat Yes 6.9 IC50 = 130 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21
CHEMBL519067 ada1a_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL583014 ada1a_human Human No 5.9 IC50 = 1320 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1
CHEMBL1306 ada1a_rat Rat Yes 4.9 IC50 = 13278 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL862 ada1a_rat Rat Yes 5.9 IC50 = 1348 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N
CHEMBL2393243 ada1a_human Human No 5.9 IC50 = 1390 nM Bind
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1
CHEMBL3040324 ada1a_human Human No 5.9 IC50 = 1390 nM Bind
Binding affinity to adrenergic alpha1A receptor (unknown origin)Binding affinity to adrenergic alpha1A receptor (unknown origin)
330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1
CHEMBL122269 ada1a_rat Rat No 7.9 IC50 = 14 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O
CHEMBL341229 ada1a_rat Rat No 7.9 IC50 = 14 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL25012 ada1a_rat Rat No 7.9 IC50 = 14 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
497 7 1 6 4.3 COc1ccccc1N1CCN(CCNC(=O)c2cccc3c(=O)c(C)c(-c4ccccc4)oc23)CC1
CHEMBL629 ada1a_rat Rat Yes 7.9 IC50 = 14 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C
CHEMBL3740558 ada1a_human Human No 7.9 IC50 = 14.3 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
467 7 0 5 4.1 CC(=O)c1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1
CHEMBL3808878 ada1a_human Human No 7.8 IC50 = 14.4 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
411 11 3 5 2.4 Cc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL315772 ada1a_human Human No 7.8 IC50 = 14.5 nM Bind
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1
CHEMBL315772 ada1a_human Human No 7.8 IC50 = 14.5 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1
CHEMBL637 ada1a_rat Rat Yes 6.9 IC50 = 140 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1
CHEMBL1201203 ada1a_rat Rat Yes 6.9 IC50 = 142 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL438151 ada1a_rat Rat Yes 6.9 IC50 = 142 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL395110 ada1a_rat Rat Yes 6.8 IC50 = 144 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1
CHEMBL3985901 ada1a_human Human No 5.8 IC50 = 1474 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
332 0 0 4 3.6 Cn1c2c(c3ccccc31)CC1c3cc4c(cc3CCN1C2)OCO4
CHEMBL122113 ada1a_rat Rat No 7.8 IC50 = 15 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
414 7 1 3 3.9 CN(CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O
CHEMBL4638599 ada1a_human Human No 7.8 IC50 = 15.1 nM Funct
Antagonist activity at alpha-1a adrenergic receptor (unknown origin)Antagonist activity at alpha-1a adrenergic receptor (unknown origin)
407 6 0 7 3.3 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccccn12
CHEMBL3742198 ada1a_human Human No 7.8 IC50 = 15.2 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3Cl)CC2)cc1
CHEMBL3810401 ada1a_human Human No 7.8 IC50 = 15.4 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
459 12 3 6 3.4 COc1cc(Cl)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL123584 ada1a_rat Rat No 6.8 IC50 = 150 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
387 5 0 4 4.0 CN1CCN(CCOc2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1
CHEMBL101055 ada1a_rat Rat No 6.8 IC50 = 150 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
277 5 1 3 3.0 COc1cccc(C(CN(C)C)C2(O)CCCCC2)c1
CHEMBL1204345 ada1a_bovin Bovine Yes 5.8 IC50 = 1500 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
456 5 1 8 2.6 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL129583 ada1a_bovin Bovine Yes 5.8 IC50 = 1500 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
456 5 1 8 2.6 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL1203296 ada1a_bovin Bovine No 4.8 IC50 = 15000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
507 7 2 7 2.5 CS(=O)(=O)Nc1ccc(CCN2CCC3(CC2)CC(=O)c2cc(NS(C)(=O)=O)ccc2O3)cc1
CHEMBL339769 ada1a_bovin Bovine No 4.8 IC50 = 15000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
507 7 2 7 2.5 CS(=O)(=O)Nc1ccc(CCN2CCC3(CC2)CC(=O)c2cc(NS(C)(=O)=O)ccc2O3)cc1
CHEMBL4102670 ada1a_human Human No 6.8 IC50 = 151 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
424 4 1 7 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2O
CHEMBL3741658 ada1a_human Human No 6.8 IC50 = 151.3 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
425 6 0 4 3.8 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3)CC2)cc1
CHEMBL2106399 ada1a_rat Rat Yes 5.8 IC50 = 1544 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
785 11 4 15 2.4 CO[C@@H]1[C@@H](O[C@@H]2O[C@H](C)[C@@H](O[C@H]3C[C@@](C)(O)[C@@H](OC(=O)CC(C)C)[C@H](C)O3)[C@H](N(C)C)[C@H]2O)[C@@H](CC=O)C[C@@H](C)[C@@H](O)/C=C/C=C/C[C@@H](C)OC(=O)C[C@H]1O
CHEMBL4083333 ada1a_human Human No 6.8 IC50 = 156 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2
CHEMBL42 ada1a_bovin Bovine Yes 6.8 IC50 = 160 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL49 ada1a_bovin Bovine Yes 4.8 IC50 = 16000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL314107 ada1a_human Human No 6.8 IC50 = 162.2 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
330 2 0 3 3.7 CN(C)CC1CC2c3cc(F)ccc3Cc3ccc(F)cc3N2O1
CHEMBL122621 ada1a_rat Rat No 4.8 IC50 = 16218.1 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
590 27 4 8 6.3 COc1cccc(CNCCCCCCNCCSSCCNCCCCCCNCc2ccccc2OC)c1
CHEMBL4209188 ada1a_human Human No 6.8 IC50 = 164 nM Funct
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1
CHEMBL118055 ada1a_human Human Yes 6.8 IC50 = 169.8 nM Bind
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1
CHEMBL125483 ada1a_rat Rat No 7.8 IC50 = 17 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL3808717 ada1a_human Human No 7.8 IC50 = 17.1 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
521 14 3 6 4.2 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1
CHEMBL430717 ada1a_bovin Bovine Yes 7.8 IC50 = 17.2 nM Bind
Binding affinity was tested on cloned bovine Alpha-1A adrenergic receptorBinding affinity was tested on cloned bovine Alpha-1A adrenergic receptor
495 8 1 9 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)COc1c(OC)cccc1C(C)C
CHEMBL4644352 ada1a_human Human No 7.8 IC50 = 17.4 nM Funct
Antagonist activity at alpha-1a adrenergic receptor (unknown origin)Antagonist activity at alpha-1a adrenergic receptor (unknown origin)
425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cccn12
CHEMBL3916182 ada1a_human Human No 7.8 IC50 = 17.6 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4
CHEMBL1112 ada1a_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL1112 ada1a_human Human Yes 6.8 IC50 = 170 nM Bind
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL1112 ada1a_human Human Yes 6.8 IC50 = 170 nM Funct
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl
CHEMBL339919 ada1a_rat Rat No 6.8 IC50 = 170 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
332 5 0 3 4.4 CN(C)CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12
CHEMBL19376 ada1a_human Human No 5.8 IC50 = 1700 nM Bind
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype.
388 4 3 8 0.9 COc1cc2nc(N3CCN[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC
CHEMBL4087132 ada1a_human Human No 6.8 IC50 = 174 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F
CHEMBL4116744 ada1a_human Human No 6.8 IC50 = 174 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F
CHEMBL1200781 ada1a_rat Rat Yes 5.8 IC50 = 1756 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21
CHEMBL549 ada1a_rat Rat Yes 5.8 IC50 = 1756 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21
CHEMBL4277101 ada1a_human Human No 6.8 IC50 = 178 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL301956 ada1a_rat Rat No 7.8 IC50 = 18 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
302 3 0 2 4.5 CN(C)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL487230 ada1a_human Human No 5.8 IC50 = 1800 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL1203233 ada1a_rat Rat No 5.7 IC50 = 1862.1 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC
CHEMBL263434 ada1a_rat Rat No 5.7 IC50 = 1862.1 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC
CHEMBL144318 ada1a_rat Rat Yes 7.7 IC50 = 19 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
424 5 1 3 4.2 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(F)ccc32)CC1
CHEMBL344335 ada1a_rat Rat No 6.7 IC50 = 190 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
322 2 0 2 5.0 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(C)CC1
CHEMBL355917 ada1a_rat Rat Yes 6.7 IC50 = 190 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
474 5 1 3 5.1 O=C1NCCN1CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C(F)(F)F)ccc32)CC1
CHEMBL99503 ada1a_rat Rat No 6.7 IC50 = 190 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
355 5 1 3 3.8 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1Br
CHEMBL81485 ada1a_human Human No 6.7 IC50 = 190.6 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1
CHEMBL154023 ada1a_human Human No 6.7 IC50 = 190.6 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1
CHEMBL156661 ada1a_human Human No 6.7 IC50 = 190.6 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1
CHEMBL19826 ada1a_human Human No 5.7 IC50 = 1900 nM Bind
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype
482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC
CHEMBL2203713 ada1a_human Human No 5.7 IC50 = 1900 nM Bind
Inhibition of alpha1A adrenergic receptorInhibition of alpha1A adrenergic receptor
326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1
CHEMBL313189 ada1a_human Human No 5.7 IC50 = 1905.5 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
308 3 0 3 3.8 CN(C)CCC1CC2c3ccccc3Cc3ccccc3N2O1
CHEMBL494155 ada1a_human Human No 5.7 IC50 = 1910 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1
CHEMBL494156 ada1a_human Human No 5.7 IC50 = 1910 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1
CHEMBL43064 ada1a_rat Rat Yes 5.7 IC50 = 1919 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
368 6 0 2 5.1 C(=C/c1ccccc1)\CN1CCN(C(c2ccccc2)c2ccccc2)CC1
CHEMBL493967 ada1a_human Human No 5.7 IC50 = 1920 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1
CHEMBL531 ada1a_rat Rat Yes 5.7 IC50 = 1930 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3
CHEMBL411 ada1a_rat Rat Yes 4.7 IC50 = 19487 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1
CHEMBL17851 ada1a_human Human No 6.7 IC50 = 199.5 nM Bind
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1
CHEMBL384790 ada1a_rat Rat No 5.7 IC50 = 1995.3 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccc(CNCCCCCCNCCSSCCNCCCCCCNCc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC
CHEMBL278865 ada1a_rat Rat Yes 8.7 IC50 = 2 nM Bind
Binding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptorBinding affinity was tested on CEC-pretreated rat hippocampus Alpha-1A adrenergic receptor
511 8 1 6 4.7 COc1ccccc1N1CCN(CC1)CCCNC(=O)c1cccc2c1oc(c1ccccc1)c(c2=O)C
CHEMBL3740019 ada1a_human Human No 8.7 IC50 = 2.0 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
439 6 0 4 4.2 Cc1ccc(N2CCN(CCc3ccc(CN4C(=O)c5ccccc5C4=O)cc3)CC2)cc1
CHEMBL3809840 ada1a_human Human No 8.7 IC50 = 2.2 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1
CHEMBL836 ada1a_human Human Yes 8.7 IC50 = 2.2 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C
CHEMBL3582269 ada1a_human Human No 8.6 IC50 = 2.5 nM Bind
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
544 5 2 13 1.6 COc1cc2nc(N3CCN(C(=O)c4cn(-c5cc6ccc(O)cc6oc5=O)nn4)CC3)nc(N)c2cc1OC
CHEMBL4170029 ada1a_rat Rat No 8.6 IC50 = 2.5 nM Bind
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
772 17 2 14 4.7 COc1cc2nc(N3CCN(C(=O)CCCCCCCCCCC(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC
CHEMBL3808511 ada1a_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
491 11 3 5 3.6 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccc(F)cc1Br
CHEMBL3808726 ada1a_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
573 13 3 6 3.8 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Br)ccc1OCC(F)(F)F
CHEMBL3809093 ada1a_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
501 14 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCc1ccccc1
CHEMBL3810346 ada1a_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
529 13 3 6 3.7 C[C@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F
CHEMBL3808896 ada1a_human Human No 8.5 IC50 = 2.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
445 12 3 6 2.3 COc1ccc(F)cc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL3809175 ada1a_human Human No 8.5 IC50 = 2.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
505 12 3 6 2.9 COc1cc(Br)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL54 ada1a_bovin Bovine Yes 7.7 IC50 = 20 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL59823 ada1a_bovin Bovine No 7.7 IC50 = 20 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
409 7 0 5 3.2 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)OCC(=O)N3C)CC1
CHEMBL3808999 ada1a_human Human No 7.7 IC50 = 20.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
423 12 3 5 3.3 CCc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL4792905 ada1a_human Human No 7.7 IC50 = 20.8 nM Funct
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
449 11 1 5 4.7 COc1ccccc1N1CCN(CCCCn2cc(CCCC(=O)O)c3ccccc32)CC1
CHEMBL61818 ada1a_bovin Bovine No 6.7 IC50 = 200 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL27991 ada1a_bovin Bovine No 5.7 IC50 = 2000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1
CHEMBL298534 ada1a_bovin Bovine No 5.7 IC50 = 2000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1
CHEMBL52438 ada1a_bovin Bovine No 5.7 IC50 = 2000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1
CHEMBL19826 ada1a_rat Rat No 5.7 IC50 = 2000 nM Bind
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtypeCompound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype
482 5 2 9 2.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@H](C(=O)NC(C)(C)C)C3)nc(N)c2cc1OC
CHEMBL11592 ada1a_bovin Bovine Yes 4.7 IC50 = 20000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 ada1a_bovin Bovine Yes 4.7 IC50 = 20000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL3984249 ada1a_human Human No 6.7 IC50 = 202.3 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
348 1 1 4 3.6 COc1cccc2[nH]c3c(c12)CC1c2cc4c(cc2CCN1C3)OCO4
CHEMBL162436 ada1a_human Human No 6.7 IC50 = 204.2 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
435 5 0 5 4.6 O=c1c(CCN2CCc3oc4ccccc4c3C2)c(Cc2ccccc2)nc2ccccn12
CHEMBL450018 ada1a_human Human No 5.7 IC50 = 2041.7 nM Bind
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1
CHEMBL99670 ada1a_rat Rat No 6.7 IC50 = 205 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
261 4 1 2 3.3 Cc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1
CHEMBL3895460 ada1a_human Human No 5.7 IC50 = 2057 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
336 0 1 3 3.7 Fc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4
CHEMBL1280 ada1a_rat Rat Yes 5.7 IC50 = 2092 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC
CHEMBL6966 ada1a_rat Rat Yes 5.7 IC50 = 2092 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC
CHEMBL3809532 ada1a_human Human No 7.7 IC50 = 21.8 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
425 11 3 5 2.7 Cc1cccc(C)c1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL1201049 ada1a_rat Rat Yes 4.7 IC50 = 21160 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL808 ada1a_rat Rat Yes 4.7 IC50 = 21160 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL165181 ada1a_human Human No 6.7 IC50 = 213.8 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
375 3 0 5 3.8 Cc1nc2ccccn2c(=O)c1CCN1CCc2sc3ccccc3c2C1
CHEMBL95523 ada1a_human Human No 6.7 IC50 = 213.8 nM Bind
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL488248 ada1a_human Human No 5.7 IC50 = 2200 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL557214 ada1a_human Human No 5.7 IC50 = 2200 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL81 ada1a_rat Rat Yes 5.7 IC50 = 2204 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O
CHEMBL83 ada1a_rat Rat Yes 4.7 IC50 = 22050 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1
CHEMBL319553 ada1a_human Human No 6.7 IC50 = 223.9 nM Bind
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1
CHEMBL6437 ada1a_rat Rat Yes 6.7 IC50 = 224 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1
CHEMBL3968227 ada1a_human Human No 6.7 IC50 = 225.3 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
392 5 1 4 4.6 CCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21
CHEMBL3740042 ada1a_human Human No 6.6 IC50 = 227.7 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
439 6 0 4 4.2 Cc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL3958316 ada1a_human Human No 5.6 IC50 = 2286 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
406 6 1 4 5.0 CCCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21
CHEMBL3740847 ada1a_human Human No 6.6 IC50 = 229.4 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
443 6 0 4 4.0 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(F)cc3)CC2)cc1
CHEMBL122018 ada1a_rat Rat No 7.6 IC50 = 23 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
400 6 1 3 3.9 CN(CCN1CCNC1=O)Cc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL157138 ada1a_rat Rat Yes 7.6 IC50 = 23 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC
CHEMBL144901 ada1a_rat Rat No 7.6 IC50 = 23 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
420 5 1 3 4.4 Cc1cccc2c(-c3ccc(F)cc3)cn(C3CCN(CCN4CCNC4=O)CC3)c12
CHEMBL522037 ada1a_human Human No 6.6 IC50 = 230 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1
CHEMBL283606 ada1a_bovin Bovine Yes 5.6 IC50 = 2300 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL1203301 ada1a_bovin Bovine No 5.6 IC50 = 2300 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
458 5 2 8 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL128745 ada1a_bovin Bovine No 5.6 IC50 = 2300 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
458 5 2 8 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(O)CC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL343444 ada1a_rat Rat Yes 5.6 IC50 = 2300 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
434 5 1 3 4.7 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(CCN2CCNC2=O)CC1
CHEMBL162232 ada1a_human Human No 6.6 IC50 = 239.9 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
387 3 0 5 4.0 Cc1cc(C)n2c(=O)c(CCN3CCc4oc5ccccc5c4C3)c(C)nc2c1
CHEMBL296419 ada1a_rat Rat Yes 7.6 IC50 = 24 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
CHEMBL726 ada1a_rat Rat Yes 7.6 IC50 = 24 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F
CHEMBL611 ada1a_rat Rat Yes 7.6 IC50 = 24 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1
CHEMBL343034 ada1a_rat Rat Yes 7.6 IC50 = 24 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
418 5 1 3 4.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1=CCN(CCN2CCNC2=O)CC1
CHEMBL487060 ada1a_human Human No 5.6 IC50 = 2400 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1
CHEMBL516 ada1a_rat Rat Yes 6.6 IC50 = 241 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1
CHEMBL162826 ada1a_human Human No 6.6 IC50 = 245.5 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
375 3 1 6 3.1 Cc1nc2c(O)cccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1
CHEMBL1631540 ada1a_rat Rat Yes 7.6 IC50 = 25.1 nM Bind
Inhibition of rat adrenergic alpha1A receptorInhibition of rat adrenergic alpha1A receptor
415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1
CHEMBL277375 ada1a_human Human No 7.6 IC50 = 25.1 nM Bind
Inhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cellsInhibitory concentration against radioligand binding to human Alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells
241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1
CHEMBL3810198 ada1a_human Human No 7.6 IC50 = 25.6 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
425 12 3 5 2.7 CCc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL3648680 ada1a_human Human Yes 5.6 IC50 = 2500 nM Bind
Antagonist activity at alpha 1a adrenergic receptor (unknown origin)Antagonist activity at alpha 1a adrenergic receptor (unknown origin)
465 4 3 8 2.9 Cn1ncc(NC(=O)c2nc(-c3c(F)cccc3F)sc2N)c1N1CC[C@@H](N)[C@H](F)CC1
CHEMBL3938121 ada1a_human Human No 6.6 IC50 = 253.8 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
336 0 1 3 3.7 Fc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4
CHEMBL163247 ada1a_human Human No 5.6 IC50 = 2570.4 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
427 3 0 5 4.7 Cc1nc2c(Cl)cc(Cl)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1
CHEMBL321364 ada1a_rat Rat No 6.6 IC50 = 260 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
325 4 1 2 3.8 CN(C)CC(c1ccccc1Br)C1(O)CCCCC1
CHEMBL305660 ada1a_rat Rat Yes 5.6 IC50 = 2605.4 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL104 ada1a_rat Rat Yes 4.6 IC50 = 26343 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL141667 ada1a_rat Rat No 7.6 IC50 = 27 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
418 5 1 3 4.3 Cc1cccc2c(-c3ccc(F)cc3)cn(C3=CCN(CCN4CCNC4=O)CC3)c12
CHEMBL13789 ada1a_human Human No 7.6 IC50 = 27.5 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1
CHEMBL3809781 ada1a_human Human No 7.6 IC50 = 27.8 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
441 11 3 7 1.9 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc2c(c1)OCO2
CHEMBL144362 ada1a_rat Rat Yes 5.6 IC50 = 2700 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
336 2 0 2 5.3 Cc1ccc2c(c1)c(-c1ccc(F)cc1)c(C)n2C1CCN(C)CC1
CHEMBL95 ada1a_rat Rat Yes 5.6 IC50 = 2749 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
198 0 1 2 2.7 Nc1c2CCCCc2nc2c1cccc2
CHEMBL567993 ada1a_human Human No 5.6 IC50 = 2790 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1
CHEMBL145712 ada1a_rat Rat Yes 6.6 IC50 = 280 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
462 6 0 3 5.5 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCN(C(C)C)C2=O)CC1
CHEMBL164612 ada1a_human Human No 6.6 IC50 = 281.8 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
393 3 0 5 4.0 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3c(Cl)cccc3c2C1
CHEMBL318544 ada1a_human Human No 6.6 IC50 = 281.8 nM Bind
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL351542 ada1a_human Human No 6.6 IC50 = 281.8 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1
CHEMBL219916 ada1a_rat Rat Yes 6.5 IC50 = 285 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2
CHEMBL162370 ada1a_human Human No 6.5 IC50 = 288.4 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
373 3 0 5 3.7 Cc1ccc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2c1
CHEMBL3967696 ada1a_human Human No 5.5 IC50 = 2880 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
424 3 1 4 5.1 c1ccc(COc2ccc3[nH]c4c(c3c2)CC2c3cc5c(cc3CCN2C4)OCO5)cc1
CHEMBL10316 ada1a_human Human Yes 5.5 IC50 = 2884.0 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
204 1 1 4 0.8 c1ccc2c(c1)OCC(C1=NCCN1)O2
CHEMBL543467 ada1a_human Human Yes 5.5 IC50 = 2884.0 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
204 1 1 4 0.8 c1ccc2c(c1)OCC(C1=NCCN1)O2
CHEMBL487064 ada1a_human Human No 5.5 IC50 = 2900 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL3187195 ada1a_human Human Yes 8.5 IC50 = 3.2 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
495 13 3 6 3.1 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCC(F)(F)F
CHEMBL3810005 ada1a_human Human No 8.5 IC50 = 3.2 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
529 13 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F
CHEMBL12713 ada1a_rat Rat Yes 8.5 IC50 = 3.4 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O
CHEMBL12713 ada1a_rat Rat Yes 8.5 IC50 = 3.4 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O
CHEMBL3809794 ada1a_human Human No 8.4 IC50 = 3.7 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
503 12 3 6 3.5 COc1cc(Br)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL3582268 ada1a_human Human No 8.4 IC50 = 3.9 nM Bind
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
477 4 2 10 2.0 COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC
CHEMBL60318 ada1a_bovin Bovine No 7.5 IC50 = 30 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21
CHEMBL61819 ada1a_bovin Bovine No 7.5 IC50 = 30 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1
CHEMBL64610 ada1a_bovin Bovine No 7.5 IC50 = 30 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL3741318 ada1a_human Human No 7.5 IC50 = 30.1 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
455 7 0 5 3.9 COc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL182150 ada1a_human Human No 6.5 IC50 = 300 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C
CHEMBL4636550 ada1a_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of adrenergic receptor alpha1a (unknown origin)Inhibition of adrenergic receptor alpha1a (unknown origin)
303 1 2 3 3.3 Cc1cc(Br)c(NC2=NCCN2)c2ccccc12
CHEMBL101056 ada1a_rat Rat No 6.5 IC50 = 300 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
291 5 1 3 3.4 COc1ccc(C(CN(C)C)C2(O)CCCCCC2)cc1
CHEMBL1119 ada1a_rat Rat Yes 6.5 IC50 = 300 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
263 5 2 3 2.7 CNCC(c1ccc(OC)cc1)C1(O)CCCCC1
CHEMBL1628258 ada1a_rat Rat Yes 6.5 IC50 = 300 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
263 5 2 3 2.7 CNCC(c1ccc(OC)cc1)C1(O)CCCCC1
CHEMBL98660 ada1a_rat Rat Yes 6.5 IC50 = 300 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
247 4 1 2 3.0 CN(C)CC(c1ccccc1)C1(O)CCCCC1
CHEMBL1178932 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL50530 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL1195096 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1
CHEMBL553833 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1
CHEMBL26018 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL300735 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL280586 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL54266 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL28312 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1
CHEMBL48925 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1
CHEMBL1203300 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
442 5 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)CCC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL338361 ada1a_bovin Bovine No 5.5 IC50 = 3000 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
442 5 1 7 3.0 CS(=O)(=O)Nc1ccc2c(c1)CCC1(CCN(CCc3ccc4nonc4c3)CC1)O2
CHEMBL567791 ada1a_human Human No 5.5 IC50 = 3000 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1
CHEMBL56 ada1a_bovin Bovine Yes 4.5 IC50 = 30000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC
CHEMBL116700 ada1a_human Human No 6.5 IC50 = 302 nM Bind
In vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblastsIn vitro binding affinity against cloned human alpha-1A-adrenoceptor receptors expressed in rat-1 fibroblasts
250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1
CHEMBL1201156 ada1a_rat Rat Yes 6.5 IC50 = 305 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL445 ada1a_rat Rat Yes 6.5 IC50 = 305 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL122384 ada1a_rat Rat No 6.5 IC50 = 310 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
344 6 0 2 5.3 CN(C)CCCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL654 ada1a_human Human Yes 5.5 IC50 = 3162.3 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1
CHEMBL3953156 ada1a_human Human No 5.5 IC50 = 3187 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@@H]1c2cc4c(cc2CCN1C3)OCO4
CHEMBL125291 ada1a_rat Rat No 7.5 IC50 = 32 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
372 5 0 3 5.3 Fc1ccc(-n2cc(OCCN3CCCCC3)c3cc(Cl)ccc32)cc1
CHEMBL728 ada1a_rat Rat Yes 7.5 IC50 = 32 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL357129 ada1a_human Human No 7.5 IC50 = 32.4 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1
CHEMBL3740351 ada1a_human Human No 7.5 IC50 = 32.4 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
469 8 0 5 4.2 CCOc1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL4788144 ada1a_human Human No 7.5 IC50 = 32.9 nM Funct
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
467 11 1 4 5.7 O=C(O)CCCc1cn(CCCCCN2CCN(c3ccccc3Cl)CC2)c2ccccc12
CHEMBL566075 ada1a_human Human No 5.5 IC50 = 3200 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C
CHEMBL3809543 ada1a_human Human No 6.5 IC50 = 324.2 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
439 11 3 5 3.1 Cc1ccc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1C
CHEMBL1909065 ada1a_rat Rat Yes 5.5 IC50 = 3337 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC
CHEMBL342730 ada1a_rat Rat No 7.5 IC50 = 34 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
420 5 1 3 4.4 Cc1cccc2c1c(-c1ccc(F)cc1)cn2C1CCN(CCN2CCNC2=O)CC1
CHEMBL3742103 ada1a_human Human No 7.5 IC50 = 34.5 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
473 6 0 4 4.8 Cc1ccc(Cl)cc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL143562 ada1a_human Human Yes 7.5 IC50 = 34.7 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1
CHEMBL19476 ada1a_rat Rat Yes 6.5 IC50 = 340 nM Bind
Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype.
522 6 2 9 3.0 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H](C1)C(=O)NC(C)(C)C)C(=O)OCc1ccccc1
CHEMBL468298 ada1a_human Human No 6.5 IC50 = 340 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1
CHEMBL3741079 ada1a_human Human No 5.5 IC50 = 3421 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
503 6 0 4 4.6 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Br)cc3)CC2)cc1
CHEMBL162501 ada1a_human Human Yes 6.5 IC50 = 346.7 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
359 3 0 5 3.4 Cc1nc2ccccn2c(=O)c1CCN1CCc2oc3ccccc3c2C1
CHEMBL49 ada1a_rat Rat Yes 5.5 IC50 = 3482 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL3805559 ada1a_human Human No 7.5 IC50 = 35 nM Bind
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1
CHEMBL155327 ada1a_human Human No 7.5 IC50 = 35.5 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1
CHEMBL523882 ada1a_human Human No 6.5 IC50 = 350 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1
CHEMBL283606 ada1a_bovin Bovine Yes 5.5 IC50 = 3500 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL1113 ada1a_rat Rat Yes 6.5 IC50 = 357 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1
CHEMBL157101 ada1a_rat Rat Yes 4.5 IC50 = 35729 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL3739762 ada1a_human Human No 7.4 IC50 = 36.1 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
450 6 0 4 4.4 [C-]#[N+]c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL99653 ada1a_rat Rat No 6.4 IC50 = 360 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
315 4 1 2 4.0 CN(C)CC(c1cccc(C(F)(F)F)c1)C1(O)CCCCC1
CHEMBL577904 ada1a_human Human No 5.4 IC50 = 3600 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptorDisplacement of [3H]prazosin from human adrenergic alpha1A receptor
403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C
CHEMBL493962 ada1a_human Human No 5.4 IC50 = 3600 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1
CHEMBL98894 ada1a_rat Rat Yes 7.4 IC50 = 37 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
315 4 1 2 4.3 CN(C)CC(c1ccc(Cl)c(Cl)c1)C1(O)CCCCC1
CHEMBL134 ada1a_rat Rat Yes 6.4 IC50 = 372 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl
CHEMBL4294617 ada1a_human Human No 6.4 IC50 = 375 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1
CHEMBL4286717 ada1a_human Human No 6.4 IC50 = 376 nM Funct
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1
CHEMBL42 ada1a_rat Rat Yes 7.4 IC50 = 38 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL762 ada1a_rat Rat Yes 7.4 IC50 = 38 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL3810187 ada1a_human Human No 7.4 IC50 = 38.2 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
523 14 3 6 3.6 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1
CHEMBL3739542 ada1a_human Human No 6.4 IC50 = 384.2 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
493 6 0 4 4.9 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccc3C(F)(F)F)CC2)cc1
CHEMBL216443 ada1a_rat Rat No 5.4 IC50 = 3890.5 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4cccc(CNCCCCCCNCCSSCCNCCCCCCNCc5cccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)c5)c4)CC3)nc(N)c2cc1OC
CHEMBL1331786 ada1a_rat Rat Yes 6.4 IC50 = 391 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N
CHEMBL420 ada1a_rat Rat Yes 6.4 IC50 = 391 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N
CHEMBL331077 ada1a_human Human No 6.4 IC50 = 398.1 nM Bind
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1
CHEMBL163190 ada1a_human Human No 6.4 IC50 = 398.1 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
373 3 0 5 3.7 Cc1nc2cccc(C)n2c(=O)c1CCN1CCc2oc3ccccc3c2C1
CHEMBL3809630 ada1a_human Human No 8.4 IC50 = 4 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
513 13 3 6 3.2 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1OCC(F)(F)F
CHEMBL4166644 ada1a_rat Rat No 8.4 IC50 = 4.3 nM Bind
Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis
513 8 1 8 3.7 COc1cc2nc(N3CCN(C(=O)Cc4ccc(OCc5ccccc5)cc4)CC3)nc(N)c2cc1OC
CHEMBL3809319 ada1a_human Human No 8.4 IC50 = 4.4 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
425 12 3 6 2.7 COc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1
CHEMBL3809600 ada1a_human Human No 8.3 IC50 = 4.6 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
445 12 3 6 2.3 COc1cc(F)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL3808408 ada1a_human Human No 8.3 IC50 = 4.8 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
427 12 3 6 2.1 COc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2
CHEMBL332365 ada1a_rat Rat No 7.4 IC50 = 40 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
316 4 0 2 4.5 CN(C)CCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12
CHEMBL418499 ada1a_bovin Bovine No 6.4 IC50 = 400 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21
CHEMBL331193 ada1a_rat Rat No 6.4 IC50 = 400 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
456 8 0 3 5.0 CC(C)N1CCN(CCN(C)CCc2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)C1=O
CHEMBL423841 ada1a_bovin Bovine No 5.4 IC50 = 4000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL54089 ada1a_bovin Bovine No 5.4 IC50 = 4000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL11592 ada1a_bovin Bovine Yes 4.4 IC50 = 40000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL301060 ada1a_bovin Bovine Yes 4.4 IC50 = 40000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL285010 ada1a_bovin Bovine No 4.4 IC50 = 40000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2
CHEMBL3948551 ada1a_human Human No 6.4 IC50 = 402.9 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
334 0 2 4 3.3 Oc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4
CHEMBL6437 ada1a_human Human Yes 6.4 IC50 = 407.4 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1
CHEMBL333774 ada1a_rat Rat No 7.4 IC50 = 41 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12)CCN1CCNC1=O
CHEMBL85735 ada1a_human Human No 7.4 IC50 = 42.7 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
308 2 0 3 3.7 Cc1ccc2c(c1)N1OC(CN(C)C)CC1c1ccccc1C2
CHEMBL453653 ada1a_human Human No 5.4 IC50 = 4200 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12
CHEMBL122042 ada1a_rat Rat No 7.4 IC50 = 43 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
428 8 1 3 4.3 CN(CCCc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O
CHEMBL329923 ada1a_rat Rat No 6.4 IC50 = 435 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
297 4 1 2 3.0 CN(C)CC(c1ccc(Br)cc1)C1(O)CCC1
CHEMBL84931 ada1a_human Human No 7.4 IC50 = 44.7 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1
CHEMBL64845 ada1a_bovin Bovine No 7.4 IC50 = 45 nM Bind
Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosinAffinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1
CHEMBL3916182 ada1a_rat Rat No 7.3 IC50 = 45.4 nM Bind
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4
CHEMBL1203232 ada1a_rat Rat No 7.3 IC50 = 45.7 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC
CHEMBL407315 ada1a_rat Rat No 7.3 IC50 = 45.7 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC
CHEMBL155326 ada1a_human Human No 7.3 IC50 = 45.7 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1
CHEMBL454642 ada1a_human Human No 5.4 IC50 = 4500 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O
CHEMBL3809314 ada1a_human Human No 6.3 IC50 = 453.9 nM Funct
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1
CHEMBL117381 ada1a_human Human Yes 6.3 IC50 = 457.1 nM Bind
In vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cellsIn vitro binding affinity against human Alpha-1A adrenergic receptor expressed in rat-1 fibroblasts cells
242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1
CHEMBL3742276 ada1a_human Human No 7.3 IC50 = 46.4 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
503 7 0 6 3.3 CS(=O)(=O)c1ccccc1N1CCN(CCc2ccc(CN3C(=O)c4ccccc4C3=O)cc2)CC1
CHEMBL3946997 ada1a_human Human Yes 6.3 IC50 = 462 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3C1C2)OCO4
CHEMBL320419 ada1a_human Human No 6.3 IC50 = 467.7 nM Bind
Concentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in humanConcentration required for 50% inhibition of binding against Alpha-1A adrenergic receptor in human
274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1
CHEMBL1203235 ada1a_rat Rat No 5.3 IC50 = 4677.4 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC
CHEMBL425267 ada1a_rat Rat No 5.3 IC50 = 4677.4 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC
CHEMBL267777 ada1a_rat Rat Yes 7.3 IC50 = 47 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F
CHEMBL267777 ada1a_rat Rat Yes 7.3 IC50 = 47 nM Bind
Compound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptorCompound was tested for i the displacement of [3H]prazosin from alpha-1 adrenergic receptor
477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F
CHEMBL267777 ada1a_rat Rat Yes 7.3 IC50 = 47 nM Bind
Compound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranesCompound was tested for the displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat striatal membranes
477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F
CHEMBL494009 ada1a_human Human No 6.3 IC50 = 470 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1
CHEMBL162682 ada1a_human Human No 6.3 IC50 = 478.6 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
485 3 0 5 4.0 Cc1nc2ccc(I)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1
CHEMBL3739533 ada1a_human Human No 7.3 IC50 = 49.6 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
426 6 0 5 3.2 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccccn3)CC2)cc1
CHEMBL468509 ada1a_human Human No 6.3 IC50 = 490 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1
CHEMBL1732 ada1a_rat Rat Yes 8.3 IC50 = 5.0 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O
CHEMBL479 ada1a_rat Rat Yes 8.3 IC50 = 5.1 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1
CHEMBL1909072 ada1a_rat Rat Yes 8.3 IC50 = 5.1 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL421244 ada1a_rat Rat No 8.2 IC50 = 5.7 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
430 8 1 4 3.8 CN(CCOc1cn(-c2ccc(F)cc2)c2ccc(Cl)cc12)CCN1CCNC1=O
CHEMBL356605 ada1a_human Human No 7.3 IC50 = 50.1 nM Bind
Binding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptorBinding affinity of compound towards Alpha-1A adrenergic receptor using membranes prepared from Rat-1 fibroblasts expressing human Alpha-1A adrenergic receptor
253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1
CHEMBL101322 ada1a_bovin Bovine No 6.3 IC50 = 500 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccn3)CC1)O2
CHEMBL1204312 ada1a_bovin Bovine No 6.3 IC50 = 500 nM Bind
Compound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligandCompound was evaluated for binding affinity at bovine brain Alpha-1 adrenergic receptor in a filtration-based assay using [3H]prazosin as the radioligand
415 5 1 6 2.5 CS(=O)(=O)Nc1ccc2c(c1)C(=O)CC1(CCN(CCc3ccccn3)CC1)O2
CHEMBL141721 ada1a_rat Rat Yes 6.3 IC50 = 500 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
323 2 0 3 3.6 Cc1ccc2c(c1)c(-c1ccc(F)cc1)cn2N1CCN(C)CC1
CHEMBL346389 ada1a_rat Rat Yes 6.3 IC50 = 500 nM Bind
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary glandInhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1
CHEMBL3403995 ada1a_human Human No 6.3 IC50 = 500 nM Bind
Inhibition of alpha-adrenoceptor 1A (unknown origin)Inhibition of alpha-adrenoceptor 1A (unknown origin)
513 13 2 7 3.5 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2OC(=O)NCc2ccccc2)C(C)C)ccc1OC
CHEMBL1183479 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL299561 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1
CHEMBL1185501 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL417550 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL283207 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL52396 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1
CHEMBL416747 ada1a_bovin Bovine No 5.3 IC50 = 5000 nM Bind
Binding affinity against alpha-1 adrenergic receptor in calf frontal cortexBinding affinity against alpha-1 adrenergic receptor in calf frontal cortex
360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1
CHEMBL263289 ada1a_rat Rat No 5.3 IC50 = 5011.9 nM Funct
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccccc4CNCCCCCCNCCSSCCNCCCCCCNCc4ccccc4C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC
CHEMBL4224703 ada1a_human Human No 6.3 IC50 = 502.1 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1
CHEMBL4302771 ada1a_human Human No 6.3 IC50 = 502.1 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1
CHEMBL319142 ada1a_rat Rat No 7.3 IC50 = 52 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
325 4 1 2 3.8 CN(C)CC(c1cccc(Br)c1)C1(O)CCCCC1
CHEMBL3582272 ada1a_human Human No 7.3 IC50 = 52.4 nM Bind
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysisDisplacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
585 9 1 13 3.1 CCN(CC)c1ccc2cc(-n3cc(CN4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)nn3)c(=O)oc2c1
CHEMBL316862 ada1a_rat Rat Yes 6.3 IC50 = 523 nM Bind
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brainInhibition of binding of [3H]imipramine to imipramine receptor in rat brain
281 4 1 2 3.7 CN(C)CC(c1ccccc1Cl)C1(O)CCCCC1
CHEMBL162058 ada1a_human Human No 5.3 IC50 = 5248.1 nM Bind
Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
419 5 0 7 3.4 COc1cc2nc(C)c(CCN3CCc4oc5ccccc5c4C3)c(=O)n2cc1OC
CHEMBL1626 ada1a_rat Rat Yes 7.3 IC50 = 53 nM Bind
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C
CHEMBL83658 ada1a_human Human No 6.3 IC50 = 537.0 nM Bind
Binding affinity against Alpha-1A adrenergic receptorBinding affinity against Alpha-1A adrenergic receptor
294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1
CHEMBL83658 ada1a_human Human No 6.3 IC50 = 537.0 nM Bind
Binding affinity for human cloned Alpha-1A adrenergic receptorBinding affinity for human cloned Alpha-1A adrenergic receptor
294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1
CHEMBL332425 ada1a_rat Rat No 7.3 IC50 = 54 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
428 8 1 3 4.3 CN(CCCN1CCNC1=O)CCc1cn(-c2ccc(F)cc2)c2cc(Cl)ccc12
CHEMBL356799 ada1a_rat Rat No 7.3 IC50 = 54 nM Bind
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranesDisplacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
422 5 1 3 4.7 CNC(=O)N(C)CCN1CCC(n2cc(-c3ccc(F)cc3)c3cc(C)ccc32)CC1
CHEMBL20734 ada1a_rat Rat Yes 6.3 IC50 = 540 nM Bind
Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranesBinding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes
387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl
CHEMBL468299 ada1a_human Human No 6.3 IC50 = 540 nM Bind
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in thymidine kinase-deficient mouse LM cells
467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1
CHEMBL490533 ada1a_human Human Yes 5.3 IC50 = 5400 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4
CHEMBL3741483 ada1a_human Human No 6.3 IC50 = 551.9 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
459 6 0 4 4.5 O=C1c2ccccc2C(=O)N1Cc1ccc(CCN2CCN(c3ccc(Cl)cc3)CC2)cc1
CHEMBL3908813 ada1a_human Human Yes 6.3 IC50 = 552.3 nM Funct
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
304 1 1 2 3.8 COc1ccc2c(c1)CCN1Cc3[nH]c4ccccc4c3CC21
CHEMBL142635 ada1a_human Human Yes 6.3 IC50 = 555 nM Bind
Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay
392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1
CHEMBL142635 ada1a_human Human Yes 6.3 IC50 = 555 nM Funct
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1
CHEMBL584606 ada1a_rat Rat No 7.3 IC50 = 56 nM Bind
Displacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 minsDisplacement of [3H]prazosin from adrenergic alpha1A receptor in Wistar rat submaxillary gland after 60 mins
367 6 1 6 2.3 C=Cc1c(C)nn(CCCN2CCN(c3ccc(C)cc3)CC2)c(=O)c1N
CHEMBL21731 ada1a_rat Rat Yes 6.3 IC50 = 567 nM Bind
DRUGMATRIX: Alph