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
CHEMBL1224527 drd1_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
295 1 3 3 3.0 C1CNCC2C1C(CC3=C2C=CC(=C3O)O)C4=CC=CC=C4
CHEMBL1224527 drd1_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
295 1 3 3 3.0 C1CNCC2C1C(CC3=C2C=CC(=C3O)O)C4=CC=CC=C4
CHEMBL415080 drd1_human Human No 9.0 EC50 = 1.0 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
350 2 3 4 2.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=C(C=C3)Br
CHEMBL315750 drd1_human Human No 8.9 EC50 = 1.3 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
291 3 3 4 2.9 CNCC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL314459 drd1_rat Rat No 8.8 EC50 = 1.7 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
277 2 3 4 2.4 C1CCC(CC1)C2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL86931 drd1_human Human Yes 8.7 EC50 = 2.0 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL86931 drd1_rat Rat Yes 8.7 EC50 = 2.0 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL87172 drd1_human Human No 7.0 EC50 = 100 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
361 4 3 4 3.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL24077 drd1_rat Rat Yes 7.0 EC50 = 100 Funct
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL101617 drd1_rat Rat No 6.0 EC50 = 1000 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
269 3 3 3 3.0 C1CC2=C(CC1NCC3=CC=CC=C3)C=CC(=C2O)O
CHEMBL41132 drd1_carau Goldfish No 8.0 EC50 = 11 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
287 0 3 4 2.6 CC1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL2335737 drd1_human Human No 8.0 EC50 = 11 Funct
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
344 1 2 3 3.6 CC1=C(C=C2C3CC(CCN3CCC2=C1)(C4=CC=C(C=C4)Cl)O)O
CHEMBL275379 drd1_human Human No 7.0 EC50 = 110 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 1.9 CC1=CN=C2CNC3CCC4=CC(=C(C=C4C3C2=C1)O)O
CHEMBL384046 drd1_human Human No 6.0 EC50 = 1100 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL384046 drd1_human Human No 6.0 EC50 = 1100 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL420788 drd1_human Human No 7.9 EC50 = 12.5 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
315 4 3 4 3.1 C#CCNCC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL284959 drd1_human Human No 6.9 EC50 = 120 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
296 0 3 4 2.3 CC1=C(N=C2CNC3CCC4=CC(=C(C=C4C3C2=C1)O)O)C
CHEMBL86669 drd1_human Human No 6.9 EC50 = 124 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
317 4 3 4 3.5 C1CCC(CC1)C2CC3=C(C=CC(=C3O)O)C(O2)CNC4CC4
CHEMBL287931 drd1_carau Goldfish No 6.9 EC50 = 125 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
355 2 3 4 4.7 C1CCC(C1)CC2=CC3=C(S2)C4C(CCC5=CC(=C(C=C45)O)O)NC3
CHEMBL15564 drd1_rat Rat Yes 4.9 EC50 = 12500 Funct
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
237 7 2 3 1.8 CCCN(CCC)CCC1=CC(=C(C=C1)O)O
CHEMBL420972 drd1_human Human No 7.9 EC50 = 13.6 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
279 6 3 4 2.9 CCCCCCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL286080 drd1_human Human Yes 6.9 EC50 = 130 Funct
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL448891 drd1_human Human Yes 5.9 EC50 = 1350 Funct
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
341 3 1 5 2.9 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)OC
CHEMBL25856 drd1_human Human No 7.9 EC50 = 14 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL25856 drd1_human Human No 7.9 EC50 = 14 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL289927 drd1_carau Goldfish No 6.9 EC50 = 140 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
358 5 3 4 5.1 CCCCCCC1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL2115213 drd1_human Human No 6.9 EC50 = 142 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
223 2 3 4 1.0 CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3099234 drd1_human Human No 6.8 EC50 = 150 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
328 4 1 5 2.3 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=NC=N4
CHEMBL1457510 drd1_human Human No 4.8 EC50 = 15970 Funct
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
325 1 1 5 2.8 COC1=C(C=CC2=C1CN3CCC4=CC5=C(C=C4C3C2)OCO5)O
CHEMBL82899 drd1_human Human No 7.8 EC50 = 16.4 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
251 2 3 4 1.8 CC(C)(C)C1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 170 Funct
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL38757 drd1_carau Goldfish No 6.8 EC50 = 170 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
343 4 3 4 4.5 CCCCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL39266 drd1_carau Goldfish No 6.8 EC50 = 170 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
308 0 3 4 3.2 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=C(S4)Cl)O)O
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 170 Funct
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL85552 drd1_human Human No 5.8 EC50 = 1740 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
335 6 4 5 2.6 C1CCC(CC1)C2CC3=C(C=CC(=C3O)O)C(O2)CNCCCO
CHEMBL27101 drd1_human Human No 7.8 EC50 = 18 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
286 0 3 5 1.9 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=CC(=N4)F)O)O
CHEMBL84983 drd1_rat Rat No 7.7 EC50 = 18.9 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
299 4 3 4 2.4 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)CCC3=CC=CC=C3
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 180 Funct
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 180 Funct
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL283247 drd1_human Human No 6.8 EC50 = 180 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
324 3 3 4 3.4 CCCCC1=CN=C2CNC3CCC4=CC(=C(C=C4C3C2=C1)O)O
CHEMBL25856 drd1_human Human No 7.7 EC50 = 19 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL25856 drd1_human Human No 7.7 EC50 = 19 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL313304 drd1_human Human No 8.7 EC50 = 2.0 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
397 2 3 4 2.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=C(C=C3)I
CHEMBL315468 drd1_human Human No 8.7 EC50 = 2.1 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL86931 drd1_human Human Yes 8.7 EC50 = 2.1 Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL587 drd1_rat Rat Yes 4.7 EC50 = 20000 Funct
Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
276 7 2 3 2.3 CCCN(CCC)CCC1=C2CC(=O)NC2=C(C=C1)O
CHEMBL3099231 drd1_human Human No 6.7 EC50 = 210 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
327 4 1 4 2.6 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC=N4
CHEMBL487387 drd1_human Human Yes 7.6 EC50 = 23 Funct
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
327 2 2 5 2.6 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
CHEMBL487387 drd1_human Human Yes 7.6 EC50 = 23 Funct
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
327 2 2 5 2.6 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
CHEMBL27117 drd1_human Human No 7.6 EC50 = 23 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 1.9 CC1=NC2=C(C=C1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL420972 drd1_rat Rat No 7.6 EC50 = 23.4 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
279 6 3 4 2.9 CCCCCCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3099235 drd1_human Human No 6.6 EC50 = 230 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
328 4 1 5 2.3 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=NC=N4
CHEMBL282136 drd1_human Human No 6.6 EC50 = 230 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 1.8 CC1=C2CNC3CCC4=CC(=C(C=C4C3C2=CN=C1)O)O
CHEMBL2114209 drd1_human Human No 6.6 EC50 = 232 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
223 2 3 4 1.0 CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL87897 drd1_human Human No 6.6 EC50 = 237 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
315 4 3 5 2.0 COC1=CC=C(C=C1)CC2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL28338 drd1_carau Goldfish Yes 7.6 EC50 = 24 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
315 2 3 4 3.4 CCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL86576 drd1_human Human No 7.6 EC50 = 24 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
301 4 3 5 1.7 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)COC3=CC=CC=C3
CHEMBL286080 drd1_human Human Yes 6.6 EC50 = 247.5 Funct
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL405519 drd1_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
261 2 2 3 3.2 CCCN1CCCC2C1CC3=C(C2)C(=C(C=C3)O)O
CHEMBL405519 drd1_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
261 2 2 3 3.2 CCCN1CCCC2C1CC3=C(C2)C(=C(C=C3)O)O
CHEMBL53 drd1_human Human Yes 7.6 EC50 = 25.7 Funct
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL315516 drd1_human Human No 5.6 EC50 = 2730 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
367 5 3 4 4.4 C1CCC(CC1)C2CC3=C(C=CC(=C3O)O)C(O2)CNCC4=CC=CC=C4
CHEMBL291100 drd1_carau Goldfish No 7.6 EC50 = 28 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
329 1 3 4 3.9 CC(C)(C)C1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL40667 drd1_carau Goldfish No 7.6 EC50 = 28 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
315 2 3 4 3.4 CCCC1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL1303 drd1_human Human Yes 7.6 EC50 = 28 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
316 6 1 3 4.9 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
CHEMBL387250 drd1_human Human No 7.5 EC50 = 29 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL446350 drd1_carau Goldfish No 7.5 EC50 = 29 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
315 1 3 4 3.4 CC(C)C1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL387250 drd1_human Human No 7.5 EC50 = 29 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL17357 drd1_rat Rat Yes 6.5 EC50 = 295 Funct
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
210 2 3 4 0.6 C1=CC(=C2C(=C1CCN)SC(=O)N2)O
CHEMBL291143 drd1_human Human Yes 8.5 EC50 = 3 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
329 2 3 4 3.0 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN
CHEMBL314459 drd1_human Human No 8.5 EC50 = 3.1 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
277 2 3 4 2.4 C1CCC(CC1)C2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL87734 drd1_human Human No 8.5 EC50 = 3.5 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
287 2 4 5 1.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC(=CC=C3)O
CHEMBL1224528 drd1_human Human No 8.4 EC50 = 3.9 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL1224528 drd1_human Human No 8.4 EC50 = 3.9 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL24077 drd1_human Human Yes 7.5 EC50 = 30 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL24077 drd1_human Human Yes 7.5 EC50 = 30 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL25856 drd1_rat Rat No 7.5 EC50 = 30 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL419680 drd1_rat Rat No 7.5 EC50 = 30.3 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
317 5 3 4 3.6 C=CCNCC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL286080 drd1_human Human Yes 6.5 EC50 = 300 Funct
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL286080 drd1_human Human Yes 6.5 EC50 = 300 Funct
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL217299 drd1_human Human Yes 7.5 EC50 = 32 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL217299 drd1_human Human Yes 7.5 EC50 = 32 Funct
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL28054 drd1_human Human No 6.5 EC50 = 320 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 1.5 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=NC=C4)O)O
CHEMBL87910 drd1_human Human No 7.5 EC50 = 34.4 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
285 3 3 4 2.0 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)CC3=CC=CC=C3
CHEMBL3099232 drd1_human Human No 6.4 EC50 = 360 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
404 5 1 4 4.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC(=N4)C5=CC=CC=C5
CHEMBL315535 drd1_human Human No 7.4 EC50 = 37.6 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
329 4 2 4 3.5 CN(CC#C)CC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL284644 drd1_human Human No 7.4 EC50 = 38 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 1.5 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=CN=C4)O)O
CHEMBL24077 drd1_human Human Yes 6.4 EC50 = 386 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL286080 drd1_human Human Yes 6.4 EC50 = 386 Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL288536 drd1_carau Goldfish No 7.4 EC50 = 39 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
273 0 3 4 2.2 C1CC2=CC(=C(C=C2C3C1NCC4=C3SC=C4)O)O
CHEMBL86576 drd1_rat Rat No 7.4 EC50 = 39.8 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
301 4 3 5 1.7 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)COC3=CC=CC=C3
CHEMBL3099233 drd1_human Human No 5.4 EC50 = 3900 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
404 5 1 4 4.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC(=N4)C5=CC=CC=C5
CHEMBL1224452 drd1_human Human No 8.4 EC50 = 4.3 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL1224452 drd1_human Human No 8.4 EC50 = 4.3 Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
269 0 3 4 1.9 C1C2C(C3=CC=CC=C3CN2)C4=CC(=C(C=C4O1)O)O
CHEMBL3099239 drd1_human Human No 6.4 EC50 = 400 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
362 4 1 4 3.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=C(C=N4)Cl
CHEMBL487387 drd1_rat Rat Yes 4.4 EC50 = 41100 Funct
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
327 2 2 5 2.6 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
CHEMBL487387 drd1_rat Rat Yes 4.4 EC50 = 41100 Funct
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
327 2 2 5 2.6 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
CHEMBL290842 drd1_carau Goldfish No 7.4 EC50 = 43 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
308 0 3 4 3.2 C1CC2=CC(=C(C=C2C3C1NCC4=C3SC(=C4)Cl)O)O
CHEMBL289867 drd1_carau Goldfish No 7.4 EC50 = 44 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
329 3 3 4 4.0 CCCCC1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL419680 drd1_human Human No 7.3 EC50 = 46.5 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
317 5 3 4 3.6 C=CCNCC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL278188 drd1_rat Rat No 5.3 EC50 = 4650 Funct
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effectDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
192 2 3 3 -0.3 C1C2=C(C=CC(=C2NC1=O)O)CCN
CHEMBL40950 drd1_carau Goldfish No 7.3 EC50 = 47 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
273 0 3 4 2.2 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=CS4)O)O
CHEMBL41809 drd1_carau Goldfish No 6.3 EC50 = 470 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
343 3 3 4 4.2 CC(C)CCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL317741 drd1_rat Rat No 6.3 EC50 = 491 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
330 3 2 3 3.9 C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Cl
CHEMBL2335736 drd1_human Human No 8.3 EC50 = 5 Funct
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
409 3 2 8 3.8 COC1=C(C=C2C3CC(CCN3CCC2=C1)(C4=CC=C(C=C4)OC(F)(F)F)O)O
CHEMBL313530 drd1_human Human No 8.3 EC50 = 5.1 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
329 2 3 4 3.0 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN
CHEMBL291143 drd1_rat Rat Yes 8.3 EC50 = 5.1 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
329 2 3 4 3.0 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN
CHEMBL84983 drd1_human Human No 8.3 EC50 = 5.2 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
299 4 3 4 2.4 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)CCC3=CC=CC=C3
CHEMBL85689 drd1_human Human No 8.2 EC50 = 5.8 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
305 2 3 4 3.5 C1CCCC(CCC1)C2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL44414 drd1_carau Goldfish No 7.3 EC50 = 50 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
301 1 3 4 3.1 CCC1=CC2=C(S1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL53 drd1_human Human Yes 7.3 EC50 = 52 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd1_human Human Yes 7.3 EC50 = 52 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL82899 drd1_rat Rat No 7.3 EC50 = 52.3 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
251 2 3 4 1.8 CC(C)(C)C1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL24077 drd1_human Human Yes 7.2 EC50 = 59 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL431220 drd1_human Human No 8.2 EC50 = 6.3 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
251 4 3 4 1.8 CCCCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL315005 drd1_human Human No 8.2 EC50 = 6.4 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
301 3 3 5 1.5 COC1=CC=CC(=C1)C2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL85409 drd1_human Human No 8.2 EC50 = 6.7 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
277 3 3 4 2.6 C1CCC(C1)CC2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL281932 drd1_human Human No 8.2 EC50 = 6.7 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 1.5 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=CC=N4)O)O
CHEMBL287513 drd1_human Human No 7.2 EC50 = 63 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
322 0 3 4 2.7 C1CCC2=NC3=C(C=C2C1)C4C(CCC5=CC(=C(C=C45)O)O)NC3
CHEMBL416435 drd1_carau Goldfish No 6.2 EC50 = 640 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
363 1 3 4 4.3 CC1=CC=CC(=C1)C2=CC3=C(S2)CNC4C3C5=CC(=C(C=C5CC4)O)O
CHEMBL84557 drd1_human Human No 6.2 EC50 = 650 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
331 5 2 4 4.0 CN(CC=C)CC1C2=C(CC(O1)C3CCCCC3)C(=C(C=C2)O)O
CHEMBL315849 drd1_human Human No 7.2 EC50 = 67 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
233 2 3 4 0.6 C#CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL420604 drd1_human Human No 7.2 EC50 = 68.7 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
263 1 3 4 1.6 C1CCC2(CC1)CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL315468 drd1_rat Rat No 8.2 EC50 = 7.1 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL25856 drd1_human Human No 8.1 EC50 = 7.2 Funct
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL25856 drd1_human Human No 8.1 EC50 = 7.2 Funct
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL407489 drd1_rat Rat No 6.2 EC50 = 700 Funct
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
247 1 3 4 1.8 C1C(C2=C(CN1)SC=C2)C3=CC(=C(C=C3)O)O
CHEMBL2331599 drd1_human Human No 6.1 EC50 = 750 Funct
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
344 1 2 3 3.6 CC1=C(C=C2C3CC(CCN3CCC2=C1)(C4=CC=C(C=C4)Cl)O)O
CHEMBL417164 drd1_carau Goldfish No 7.1 EC50 = 77 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
329 3 3 4 4.0 CCCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL41196 drd1_carau Goldfish No 7.1 EC50 = 79 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
355 1 3 4 4.4 C1CCC(CC1)C2=CC3=C(S2)C4C(CCC5=CC(=C(C=C45)O)O)NC3
CHEMBL2335740 drd1_human Human No 8.1 EC50 = 8 Funct
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
360 2 2 4 3.2 COC1=C(C=C2C3CC(CCN3CCC2=C1)(C4=CC=C(C=C4)Cl)O)O
CHEMBL291143 drd1_carau Goldfish Yes 8.1 EC50 = 8.2 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
329 2 3 4 3.0 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN
CHEMBL313530 drd1_rat Rat No 8.1 EC50 = 8.3 Funct
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
329 2 3 4 3.0 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN
CHEMBL26965 drd1_human Human No 8.1 EC50 = 8.6 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
310 2 3 4 2.7 CCCC1=NC2=C(C=C1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL285924 drd1_human Human No 8.1 EC50 = 8.8 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
298 1 3 5 1.8 COC1=NC2=C(C=C1)C3C(CCC4=CC(=C(C=C34)O)O)NC2
CHEMBL43514 drd1_carau Goldfish No 7.1 EC50 = 80 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
349 1 3 4 3.9 C1CC2=CC(=C(C=C2C3C1NCC4=C3C=C(S4)C5=CC=CC=C5)O)O
CHEMBL26365 drd1_human Human No 6.1 EC50 = 800 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
286 0 3 5 1.6 C1CC2=CC(=C(C=C2C3C1NCC4=C(C=NC=C34)F)O)O
CHEMBL83080 drd1_human Human Yes 5.1 EC50 = 8577 Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL83080 drd1_human Human Yes 5.1 EC50 = 8580 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL288846 drd1_carau Goldfish No 7.1 EC50 = 88 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
329 2 3 4 3.9 CC(C)CC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL25856 drd1_carau Goldfish No 7.1 EC50 = 88 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL3099230 drd1_human Human No 7.1 EC50 = 89 Funct
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
327 4 1 4 2.6 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC=N4
CHEMBL86325 drd1_human Human No 7.1 EC50 = 89 Funct
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
315 5 3 5 1.4 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)COCC3=CC=CC=C3
CHEMBL28338 drd1_human Human Yes 8.1 EC50 = 9 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
315 2 3 4 3.4 CCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL28338 drd1_human Human Yes 8.1 EC50 = 9 Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
315 2 3 4 3.4 CCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL290149 drd1_carau Goldfish No 7.0 EC50 = 94 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
355 1 3 4 4.4 C1CCC(CC1)C2=CC3=C(S2)CNC4C3C5=CC(=C(C=C5CC4)O)O
CHEMBL24077 drd1_carau Goldfish Yes 6.0 EC50 = 950 Funct
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL136190 drd1_rat Rat No 9.4 IC50 = 0.4 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
316 1 1 2 5.0 CC1C(C2=CC(=C(C=C2CCN1C)Cl)O)(C)C3=CC=CC=C3
CHEMBL62 drd1_rat Rat Yes 9.2 IC50 = 0.6 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.2 IC50 = 0.7 Funct
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.7 Funct
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.7 Funct
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136226 drd1_rat Rat No 9.1 IC50 = 0.8 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
361 2 0 3 4.4 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CSC=C4)C
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.8 Funct
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.8 Funct
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136235 drd1_rat Rat No 9.1 IC50 = 0.9 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
356 2 0 4 4.3 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)F)C4=CC=C(C=C4)F)C
CHEMBL344206 drd1_rat Rat No 9.1 IC50 = 0.9 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
385 2 0 3 4.9 CN1CCN(CC12CCC2)C3CC(C4=C3C=C(C=C4)Cl)C5=CC=C(C=C5)F
CHEMBL62 drd1_human Human Yes 9.0 IC50 = 1.0 Funct
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL343922 drd1_rat Rat No 9.0 IC50 = 1.0 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
399 2 0 3 5.3 CN1CCN(CC12CCCC2)C3CC(C4=C3C=C(C=C4)Cl)C5=CC=C(C=C5)F
CHEMBL62 drd1_human Human Yes 9.0 IC50 = 1.0 Funct
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136340 drd1_rat Rat No 9.0 IC50 = 1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
403 4 1 4 4.1 CC1(CN(CCN1CCO)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL62 drd1_rat Rat Yes 9.0 IC50 = 1 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.0 IC50 = 1.0 Funct
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136683 drd1_rat Rat No 9.0 IC50 = 1.1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
359 2 1 3 4.3 CC1(CN(CCN1)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL136932 drd1_rat Rat No 9.0 IC50 = 1.1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
417 5 1 4 4.5 CC1(CN(CCN1CCCO)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL137960 drd1_rat Rat No 9.0 IC50 = 1.1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
355 2 0 2 4.7 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=CC=C4)C
CHEMBL64875 drd1_rat Rat No 8.9 IC50 = 1.2 Funct
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL64875 drd1_rat Rat No 8.9 IC50 = 1.2 Funct
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL267723 drd1_rat Rat Yes 8.9 IC50 = 1.2 Funct
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
404 5 2 4 2.3 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2O)I)OC
CHEMBL62 drd1_rat Rat Yes 8.9 IC50 = 1.3 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 8.9 IC50 = 1.4 Funct
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL343078 drd1_rat Rat No 8.8 IC50 = 1.5 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
406 2 0 6 5.1 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)F)C
CHEMBL136776 drd1_rat Rat No 8.8 IC50 = 1.8 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
417 2 0 3 4.9 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Br)C4=CC=C(C=C4)F)C
CHEMBL136822 drd1_rat Rat No 8.7 IC50 = 1.9 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
429 4 1 4 4.6 C1CCC2(C1)CN(CCN2CCO)C3CC(C4=C3C=C(C=C4)Cl)C5=CC=C(C=C5)F
CHEMBL32145 drd1_rat Rat Yes 8.0 IC50 = 10.1 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
374 3 2 3 4.3 C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Br
CHEMBL452510 drd1_rat Rat Yes 7.0 IC50 = 100 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)OC)O
CHEMBL73589 drd1_rat Rat No 7.0 IC50 = 100 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
457 3 0 9 3.7 CN1CCN(CC1)C2=NC3=CC=CC=C3SC4=C2C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL452510 drd1_rat Rat Yes 7.0 IC50 = 100 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)OC)O
CHEMBL452512 drd1_rat Rat No 6.0 IC50 = 1000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=C(C(=C(C=C4)OC)O)OC3=C(C=C2)O
CHEMBL452512 drd1_rat Rat No 6.0 IC50 = 1000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=C(C(=C(C=C4)OC)O)OC3=C(C=C2)O
CHEMBL27650 drd1_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
429 8 0 5 4.2 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL50188 drd1_bovin Bovine No 5.0 IC50 = 10000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
429 8 0 5 4.2 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL329444 drd1_rat Rat No 5.0 IC50 = 10000 Funct
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
249 2 1 4 1.6 CCCN1CCC2=C(C1)CCC3=C2N=C(S3)N
CHEMBL93428 drd1_rat Rat Yes 5.0 IC50 = 10000 Funct
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
223 3 1 4 1.7 CCCN1CCC=C(C1)C2=CSC(=N2)N
CHEMBL27763 drd1_bovin Bovine No 4.0 IC50 = 100000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
429 8 1 5 4.3 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4O)OC3
CHEMBL284912 drd1_bovin Bovine No 4.0 IC50 = 100000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
363 9 0 5 3.3 CCCN(CCCCN1CCOCC1)C2CC3=C(C=CC=C3OC)OC2
CHEMBL27995 drd1_bovin Bovine Yes 4.0 IC50 = 100000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
249 5 1 3 3.5 CCCN(CCC)C1CC2=C(C=CC=C2O)OC1
CHEMBL283606 drd1_bovin Bovine Yes 4.0 IC50 = 100000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
263 6 0 3 3.8 CCCN(CCC)C1CC2=C(C=CC=C2OC)OC1
CHEMBL416747 drd1_bovin Bovine No 4.0 IC50 = 100000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
361 9 0 4 4.5 CCCN(CCCCN1CCCCC1)C2CC3=C(C=CC=C3OC)OC2
CHEMBL137478 drd1_bovin Bovine No 4.0 IC50 = 100000 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
275 3 0 3 3.6 CCCN1CCCCC12CC3=C(C=CC=C3OC)OC2
CHEMBL283606 drd1_bovin Bovine Yes 4.0 IC50 = 100000 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
263 6 0 3 3.8 CCCN(CCC)C1CC2=C(C=CC=C2OC)OC1
CHEMBL113477 drd1_rat Rat No 7.0 IC50 = 102 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
251 0 2 2 2.9 C1CC2=C(C=C(C=C2)O)C3C1NCC4=CC=CC=C34
CHEMBL42 drd1_human Human Yes 7.0 IC50 = 107 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL119455 drd1_rat Rat No 7.0 IC50 = 107 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
251 0 1 2 2.7 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O
CHEMBL284746 drd1_rat Rat Yes 5.0 IC50 = 10700 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL1201356 drd1_human Human Yes 6.0 IC50 = 1077 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
339 4 3 3 2.3 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C
CHEMBL1201356 drd1_human Human Yes 6.0 IC50 = 1077 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
339 4 3 3 2.3 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C
CHEMBL1108 drd1_human Human Yes 6.0 IC50 = 1092 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
379 6 1 4 3.5 C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL1108 drd1_human Human Yes 6.0 IC50 = 1092 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
379 6 1 4 3.5 C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
CHEMBL415300 drd1_rat Rat Yes 8.0 IC50 = 11 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
327 1 1 3 3.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)Cl
CHEMBL415300 drd1_rat Rat Yes 8.0 IC50 = 11 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
327 1 1 3 3.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)Cl
CHEMBL25856 drd1_rat Rat No 7.9 IC50 = 11.6 Funct
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL54 drd1_human Human Yes 7.0 IC50 = 110 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL119455 drd1_rat Rat No 7.0 IC50 = 110 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
251 0 1 2 2.7 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O
CHEMBL54 drd1_human Human Yes 7.0 IC50 = 110 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL119455 drd1_rat Rat No 7.0 IC50 = 110 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
251 0 1 2 2.7 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O
CHEMBL2203622 drd1_human Human No 6.0 IC50 = 1100 Funct
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
298 0 0 3 3.8 CN1C2=CN=C1OCCC=CCCCCOC3=CC=CC=C32
CHEMBL415 drd1_human Human Yes 6.0 IC50 = 1113 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
315 4 0 2 5.2 CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl
CHEMBL415 drd1_human Human Yes 6.0 IC50 = 1113 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
315 4 0 2 5.2 CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl
CHEMBL82706 drd1_rat Rat No 6.0 IC50 = 1120 Funct
Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.
243 4 3 3 2.3 C1=CC=C(C=C1)CC(CN)C2=CC(=C(C=C2)O)O
CHEMBL326263 drd1_human Human No 6.0 IC50 = 1120 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
504 10 0 6 5.9 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)OCCC4=CC=C(C=C4)C#N
CHEMBL2057442 drd1_human Human No 6.9 IC50 = 113.8 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
385 5 1 6 2.4 COC1=CC(=C(C2=C1CN3CCC4=CC(=C(C=C4C3C2)OC)OC)CO)OC
CHEMBL2057441 drd1_human Human No 6.9 IC50 = 113.8 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
355 4 0 5 3.2 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)OC
CHEMBL133615 drd1_rat Rat No 6.0 IC50 = 1130 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
369 2 1 2 3.8 C1CC2C(CCC3=C2C=CC=C3O)N(C1)CC=CI
CHEMBL111348 drd1_rat Rat No 6.9 IC50 = 115 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
265 0 1 2 3.3 CN1CC2=CC=CC=C2C3C1CCC4=C3C=C(C=C4)O
CHEMBL2057446 drd1_human Human No 4.9 IC50 = 11840 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
385 5 0 6 3.2 COC1=CC(=C2CN3CCC4=CC(=C(C(=C4C3CC2=C1)OC)OC)OC)OC
CHEMBL2057446 drd1_human Human No 4.9 IC50 = 11840 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
385 5 0 6 3.2 COC1=CC(=C2CN3CCC4=CC(=C(C(=C4C3CC2=C1)OC)OC)OC)OC
CHEMBL508112 drd1_human Human Yes 5.9 IC50 = 1189 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
332 3 0 6 5.6 C1=CC=C2C(=C1)N=C(S2)SSC3=NC4=CC=CC=C4S3
CHEMBL508112 drd1_human Human Yes 5.9 IC50 = 1189 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
332 3 0 6 5.6 C1=CC=C2C(=C1)N=C(S2)SSC3=NC4=CC=CC=C4S3
CHEMBL305660 drd1_human Human Yes 5.9 IC50 = 1192.9 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
470 10 0 3 7.2 CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL305660 drd1_human Human Yes 5.9 IC50 = 1192.9 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
470 10 0 3 7.2 CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
CHEMBL317982 drd1_rat Rat No 7.9 IC50 = 12 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
342 2 0 2 5.0 CN1CCC(CC1)C2=CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL25856 drd1_rat Rat No 7.9 IC50 = 12 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL487387 drd1_human Human Yes 7.9 IC50 = 12.3 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
327 2 2 5 2.6 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
CHEMBL407489 drd1_rat Rat No 6.9 IC50 = 120 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
247 1 3 4 1.8 C1C(C2=C(CN1)SC=C2)C3=CC(=C(C=C3)O)O
CHEMBL132304 drd1_rat Rat No 6.9 IC50 = 120 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
369 2 1 2 3.9 C1CC2CC3=C(CC2N(C1)CC=CI)C=CC=C3O
CHEMBL170974 drd1_rat Rat No 5.9 IC50 = 1200 Funct
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
277 2 0 1 4.6 C1CC2CC3=CC=CC=C3CC2N(C1)CC4=CC=CC=C4
CHEMBL8412 drd1_bovin Bovine Yes 4.9 IC50 = 12000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
401 6 0 7 1.5 C1CN(CCN1CCCCN2C(=O)C3=CC=CC=C3S2(=O)=O)C4=NC=CC=N4
CHEMBL8412 drd1_bovin Bovine Yes 4.9 IC50 = 12000 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
401 6 0 7 1.5 C1CN(CCN1CCCCN2C(=O)C3=CC=CC=C3S2(=O)=O)C4=NC=CC=N4
CHEMBL155246 drd1_rat Rat No 4.9 IC50 = 12100 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
265 1 0 2 3.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC
CHEMBL14239 drd1_rat Rat No 5.9 IC50 = 1230 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
356 2 3 3 2.7 CC(=O)NC(=S)NCC1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)C
CHEMBL257958 drd1_rat Rat Yes 4.9 IC50 = 12500 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
337 2 2 5 0.9 CC1(C2=CC(=O)C=CC2=C3C4=C1NC=CC4=C(C(=C3O)OC)OC)C
CHEMBL257958 drd1_rat Rat Yes 4.9 IC50 = 12500 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
337 2 2 5 0.9 CC1(C2=CC(=O)C=CC2=C3C4=C1NC=CC4=C(C(=C3O)OC)OC)C
CHEMBL608530 drd1_human Human No 5.9 IC50 = 1251 Funct
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
387 4 0 5 4.5 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C
CHEMBL608530 drd1_human Human No 5.9 IC50 = 1251 Funct
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
387 4 0 5 4.5 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C
CHEMBL584 drd1_human Human Yes 4.9 IC50 = 12935 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
568 10 4 6 5.7 CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O
CHEMBL584 drd1_human Human Yes 4.9 IC50 = 12935 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
568 10 4 6 5.7 CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O
CHEMBL344680 drd1_rat Rat No 7.9 IC50 = 13 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
320 2 0 2 4.1 CC1(CN(CCN1C)C2CC(C3=CC=CC=C23)C4=CC=CC=C4)C
CHEMBL138745 drd1_rat Rat No 7.9 IC50 = 13 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 5.0 CC1CN(CC(N1C)C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL96618 drd1_rat Rat No 6.9 IC50 = 130 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
375 4 1 4 3.5 C1CN(CCN1CCO)C2CC(C3=C2C(=CC=C3)Cl)C4=CC=C(C=C4)F
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL106622 drd1_rat Rat No 5.9 IC50 = 1300 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 2 2 4 3.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C(=C(C=C4)O)O
CHEMBL479 drd1_rat Rat Yes 5.9 IC50 = 1300 Funct
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL106622 drd1_rat Rat No 5.9 IC50 = 1300 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
313 2 2 4 3.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C(=C(C=C4)O)O
CHEMBL106622 drd1_rat Rat No 5.9 IC50 = 1300 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 2 2 4 3.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C(=C(C=C4)O)O
CHEMBL73082 drd1_rat Rat No 6.9 IC50 = 133 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
365 1 0 2 5.6 CC(=C1C2=C(C=C(C=C2)Cl)C(=CC3=CC=CC=C31)N4CCN(CC4)C)C
CHEMBL38848 drd1_rat Rat No 5.9 IC50 = 1330 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
255 4 0 1 4.6 CC(=CCN1CCCC(C1)C=CC2=CC=CC=C2)C
CHEMBL154709 drd1_rat Rat Yes 4.9 IC50 = 13300 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
281 1 1 3 2.6 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OC)O
CHEMBL611207 drd1_human Human No 6.9 IC50 = 137 Funct
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
387 4 0 5 4.5 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C
CHEMBL150550 drd1_rat Rat No 6.9 IC50 = 138.4 Funct
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
249 2 1 4 2.2 CCCN1CCC=C2C1CCC3=C2N=C(S3)N
CHEMBL2057455 drd1_human Human No 5.9 IC50 = 1380 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
341 3 1 5 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)OC
CHEMBL2057455 drd1_human Human No 5.9 IC50 = 1380 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
341 3 1 5 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)OC
CHEMBL417608 drd1_human Human No 4.9 IC50 = 13803.8 Funct
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
457 10 0 5 4.8 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC3CC4=C(C=CC=C4OC)OC3
CHEMBL2057445 drd1_human Human No 7.8 IC50 = 14.3 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
355 4 0 5 3.2 COC1=CC(=C2C3CC4=CC(=CC(=C4CN3CCC2=C1)OC)OC)OC
CHEMBL2334881 drd1_human Human No 7.8 IC50 = 14.7 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
339 1 1 5 2.7 COC1=C(C=CC2=C1CN3CCC4=CC5=C(C=C4C3C2)OCCO5)O
CHEMBL2057455 drd1_human Human No 5.9 IC50 = 1400 Funct
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
341 3 1 5 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)OC
CHEMBL2057443 drd1_human Human No 6.9 IC50 = 141.6 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
339 2 0 5 3.1 COC1=CC(=C2CN3CCC4=CC5=C(C=C4C3CC2=C1)OCO5)OC
CHEMBL2057443 drd1_human Human No 6.9 IC50 = 141.6 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
339 2 0 5 3.1 COC1=CC(=C2CN3CCC4=CC5=C(C=C4C3CC2=C1)OCO5)OC
CHEMBL13816 drd1_rat Rat No 5.9 IC50 = 1420 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
389 5 2 3 3.8 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CNC(=O)OCC5=CC=CC=C5
CHEMBL192037 drd1_rat Rat No 4.8 IC50 = 14500 Funct
Compound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranesCompound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranes
220 5 0 1 2.9 CCCN(CCC)C1CCN2C=CC=C2C1
CHEMBL461571 drd1_human Human No 5.8 IC50 = 1530 Funct
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
532 8 1 8 7.1 CC1=C(C2=C(N1CC3=CC(=CC=C3)OC(C)C(=O)O)C=C(C=C2)OC(F)(F)F)C(=O)C4=CC=C(C=C4)Cl
CHEMBL461571 drd1_human Human No 5.8 IC50 = 1530 Funct
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
532 8 1 8 7.1 CC1=C(C2=C(N1CC3=CC(=CC=C3)OC(C)C(=O)O)C=C(C=C2)OC(F)(F)F)C(=O)C4=CC=C(C=C4)Cl
CHEMBL1626 drd1_human Human Yes 5.8 IC50 = 1535 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
344 6 0 2 5.0 CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C
CHEMBL1626 drd1_human Human Yes 5.8 IC50 = 1535 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
344 6 0 2 5.0 CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C
CHEMBL728 drd1_human Human Yes 6.8 IC50 = 155 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL728 drd1_human Human Yes 6.8 IC50 = 155 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
374 4 0 4 4.9 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL37661 drd1_rat Rat No 5.8 IC50 = 1550 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
305 6 0 1 5.5 C1CC(CN(C1)CCCC2=CC=CC=C2)C=CC3=CC=CC=C3
CHEMBL136562 drd1_rat Rat No 7.8 IC50 = 16 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
358 4 1 5 3.0 C1CN(CCN1CCO)C2CC(C3=C2C=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL136553 drd1_rat Rat No 7.8 IC50 = 16 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
327 2 0 2 4.1 CN1CCN(CC1)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=CC=C4
CHEMBL57029 drd1_rat Rat No 5.8 IC50 = 1650 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
355 6 1 4 3.6 CC1CN(CCC1(C2=CC=CC=C2)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL49995 drd1_rat Rat No 4.8 IC50 = 16600 Funct
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
297 4 2 3 4.0 CCCN1CCC2=CC(=C(C=C2C1CC3=CC=CC=C3)O)O
CHEMBL326781 drd1_rat Rat No 4.8 IC50 = 16700 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
251 0 2 2 2.9 C1CC2=C(C=C(C=C2)O)C3C1NCC4=CC=CC=C34
CHEMBL137430 drd1_rat Rat No 7.8 IC50 = 17 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
378 2 0 6 4.4 CN1CCN(CC1)C2CC(C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)F
CHEMBL479 drd1_rat Rat Yes 7.8 IC50 = 17.3 Funct
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL155884 drd1_rat Rat No 6.8 IC50 = 170 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)Br)O
CHEMBL155884 drd1_rat Rat No 6.8 IC50 = 170 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)Br)O
CHEMBL1358628 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1358628 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL1729 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL74656 drd1_human Human Yes 5.8 IC50 = 1700 Funct
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
466 9 2 7 3.4 COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
CHEMBL155884 drd1_rat Rat No 6.8 IC50 = 171 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)Br)O
CHEMBL288096 drd1_rat Rat No 5.8 IC50 = 1720 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
311 2 3 4 2.8 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)O)C(=C(C=C4)O)O
CHEMBL288096 drd1_rat Rat No 5.8 IC50 = 1720 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
311 2 3 4 2.8 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)O)C(=C(C=C4)O)O
CHEMBL257747 drd1_rat Rat No 4.8 IC50 = 17200 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
311 2 1 4 3.1 CN1CCC2=C(C(=C(C3=C2C1CC4=CC=CC=C43)O)OC)OC
CHEMBL257747 drd1_rat Rat No 4.8 IC50 = 17200 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
311 2 1 4 3.1 CN1CCC2=C(C(=C(C3=C2C1CC4=CC=CC=C43)O)OC)OC
CHEMBL1457510 drd1_human Human No 4.8 IC50 = 17370 Funct
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
325 1 1 5 2.8 COC1=C(C=CC2=C1CN3CCC4=CC5=C(C=C4C3C2)OCO5)O
CHEMBL92560 drd1_rat Rat No 5.8 IC50 = 1800 Funct
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
375 4 1 4 3.5 C1CN(CCN1CCO)C2CC(C3=C2C=CC(=C3)Cl)C4=CC=C(C=C4)F
CHEMBL155833 drd1_rat Rat No 6.7 IC50 = 181 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C(C=CC(=C43)O)Br
CHEMBL2057441 drd1_human Human No 6.7 IC50 = 189.0 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
355 4 0 5 3.2 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)OC
CHEMBL286424 drd1_rat Rat No 5.7 IC50 = 1880 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
374 3 2 3 4.3 C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Br
CHEMBL342698 drd1_rat Rat No 7.7 IC50 = 19 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 5.0 CC1CN(C(CN1C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C)C
CHEMBL95636 drd1_rat Rat Yes 7.7 IC50 = 19 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
408 4 1 7 3.7 C1CN(CCN1CCO)C2CC(C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)F
CHEMBL288090 drd1_rat Rat Yes 7.7 IC50 = 19.7 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
295 3 2 3 3.6 C=CCN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O
CHEMBL286080 drd1_rat Rat Yes 6.7 IC50 = 190 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL269160 drd1_rat Rat No 6.7 IC50 = 190 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
352 2 2 4 2.6 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)C(=O)NC5=NC=CS5
CHEMBL336128 drd1_rat Rat No 5.7 IC50 = 1900 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
353 2 0 1 4.1 C1CC2C(CCC3=CC=CC=C23)N(C1)CC=CI
CHEMBL42 drd1_rat Rat Yes 6.7 IC50 = 192 Funct
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL42 drd1_rat Rat Yes 6.7 IC50 = 192 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
327 1 1 4 3.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
CHEMBL479 drd1_human Human Yes 6.7 IC50 = 194 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL479 drd1_human Human Yes 6.7 IC50 = 194 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL413105 drd1_rat Rat Yes 4.7 IC50 = 19700 Funct
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
214 1 1 1 2.8 CN(C)C1CCC2=C(C1)C3=C(C=C2)NC=C3
CHEMBL7002 drd1_human Human Yes 4.7 IC50 = 19785 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
333 5 1 4 4.8 CC1(CCCCC1)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
CHEMBL7002 drd1_human Human Yes 4.7 IC50 = 19785 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
333 5 1 4 4.8 CC1(CCCCC1)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
CHEMBL574700 drd1_human Human No 4.7 IC50 = 19800 Funct
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
611 11 2 8 5.4 CC1=CC=CC=C1C2CN(CCC3=CC(=C(C=C23)O)O)CCCN4C=C(N=N4)CCCN5CCN(CC5)C6=CC=CC=C6OC
CHEMBL574700 drd1_human Human No 4.7 IC50 = 19800 Funct
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
611 11 2 8 5.4 CC1=CC=CC=C1C2CN(CCC3=CC(=C(C=C23)O)O)CCCN4C=C(N=N4)CCCN5CCN(CC5)C6=CC=CC=C6OC
CHEMBL140189 drd1_rat Rat No 8.7 IC50 = 2.1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
352 2 0 3 4.5 CC1=CC2=C(C=C1)C(CC2N3CCN(C(C3)(C)C)C)C4=CC=C(C=C4)F
CHEMBL335155 drd1_rat Rat No 8.7 IC50 = 2.1 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
385 2 0 3 5.1 C1CCN2CCN(CC2C1)C3CC(C4=C3C=C(C=C4)Cl)C5=CC=C(C=C5)F
CHEMBL279634 drd1_rat Rat No 8.7 IC50 = 2.1 Funct
Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.
345 2 1 4 5.4 CN1CCC2=CC(=C(C=C2C(C1)C3=CC(=CC=C3)N=C=S)O)Cl
CHEMBL71 drd1_rat Rat Yes 8.7 IC50 = 2.2 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL303313 drd1_rat Rat Yes 8.7 IC50 = 2.2 Funct
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL64249 drd1_rat Rat Yes 8.7 IC50 = 2.2 Funct
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL303313 drd1_rat Rat Yes 8.7 IC50 = 2.2 Funct
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL303313 drd1_rat Rat Yes 8.7 IC50 = 2.2 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
345 1 0 3 4.3 CN1CCN(CC1)C2CC3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL344216 drd1_rat Rat No 8.6 IC50 = 2.4 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
359 2 0 3 4.6 CC1CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL136722 drd1_rat Rat No 8.6 IC50 = 2.5 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
338 2 0 3 4.2 CC1(CN(CCN1C)C2CC(C3=CC=CC=C23)C4=CC=C(C=C4)F)C
CHEMBL62 drd1_human Human Yes 8.6 IC50 = 2.5 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136648 drd1_rat Rat No 8.6 IC50 = 2.8 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
392 2 1 6 4.6 CC1(CN(CCN1)C2CC(C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)F)C
CHEMBL70319 drd1_rat Rat Yes 6.7 IC50 = 200 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
475 3 1 10 3.7 CN1CCN(CC1)C2=C3C=C(C=CC3=NC4=C(N2)C=C(C=C4)Cl)OS(=O)(=O)C(F)(F)F
CHEMBL92896 drd1_rat Rat No 5.7 IC50 = 2000 Funct
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
375 4 1 4 3.5 C1CN(CCN1CCO)C2CC(C3=C2C=CC=C3Cl)C4=CC=C(C=C4)F
CHEMBL27991 drd1_bovin Bovine No 4.7 IC50 = 20000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
415 10 1 5 4.7 CCCN(CCCCNC(=O)C1=CC=C(C=C1)F)C2CC3=C(C=CC=C3OC)OC2
CHEMBL298534 drd1_bovin Bovine No 4.7 IC50 = 20000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
415 10 1 5 4.7 CCCN(CCCCNC(=O)C1=CC=C(C=C1)F)C2CC3=C(C=CC=C3OC)OC2
CHEMBL28287 drd1_bovin Bovine No 4.7 IC50 = 20000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
445 9 0 6 4.3 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL50722 drd1_bovin Bovine No 4.7 IC50 = 20000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
445 9 0 6 4.3 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL23529 drd1_rat Rat Yes 4.7 IC50 = 20000 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
276 1 1 1 3.9 CN1CCC2=C(C(C1)C3=CC=CC=C3)NC4=CC=CC=C24
CHEMBL3344459 drd1_human Human No 5.7 IC50 = 2010 Funct
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
343 3 1 4 4.3 CC(C)CC1=CC2=C(S1)CC3C4=CC(=C(C=C4CCN3C2)OC)O
CHEMBL3344459 drd1_human Human No 5.7 IC50 = 2010 Funct
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
343 3 1 4 4.3 CC(C)CC1=CC2=C(S1)CC3C4=CC(=C(C=C4CCN3C2)OC)O
CHEMBL91453 drd1_rat Rat Yes 6.7 IC50 = 203.1 Funct
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
249 2 1 4 2.2 CCCN1CCC=C2C1CCC3=C2N=C(S3)N
CHEMBL303339 drd1_rat Rat No 4.7 IC50 = 20400 Funct
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
214 1 1 1 2.8 CN(C)C1CCC2=C(C1)C3=C(C=C2)NC=C3
CHEMBL1479 drd1_human Human Yes 4.7 IC50 = 20449 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
337 1 1 3 3.8 CC12CCC3C(C1CCC2(C#C)O)CCC4=CC5=C(CC34C)C=NO5
CHEMBL1479 drd1_human Human Yes 4.7 IC50 = 20449 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
337 1 1 3 3.8 CC12CCC3C(C1CCC2(C#C)O)CCC4=CC5=C(CC34C)C=NO5
CHEMBL388564 drd1_rat Rat Yes 6.7 IC50 = 206 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
485 2 2 5 4.1 CN1CCC2=C(C(=C(C3=C2C1CC4=C(C(=C(C=C43)OC)O)Br)OC)O)Br
CHEMBL388564 drd1_rat Rat Yes 6.7 IC50 = 206 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
485 2 2 5 4.1 CN1CCC2=C(C(=C(C3=C2C1CC4=C(C(=C(C=C43)OC)O)Br)OC)O)Br
CHEMBL72162 drd1_rat Rat No 7.7 IC50 = 21 Funct
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
337 1 0 2 4.7 CN1CCN(CC1)C2=CC3=CC=CC=C3C(=C)C4=C2C=C(C=C4)Cl
CHEMBL91310 drd1_rat Rat No 7.7 IC50 = 21 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
302 1 0 2 4.1 CN1CCN(CC1)C2=CC3=CC=CC=C3C(=C)C4=CC=CC=C42
CHEMBL136841 drd1_rat Rat No 6.7 IC50 = 210 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
370 5 1 5 2.8 COC1=CC2=C(C=C1)C(CC2N3CCN(CC3)CCO)C4=CC=C(C=C4)F
CHEMBL307163 drd1_rat Rat No 5.7 IC50 = 2100 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
386 3 1 6 2.0 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)OS(=O)(=O)C
CHEMBL448891 drd1_human Human Yes 4.7 IC50 = 21270 Funct
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
341 3 1 5 2.9 COC1=C(C=C2C3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)OC
CHEMBL964 drd1_human Human Yes 5.7 IC50 = 2158 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
297 7 0 4 3.9 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL964 drd1_human Human Yes 5.7 IC50 = 2158 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
297 7 0 4 3.9 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL84639 drd1_rat Rat Yes 4.7 IC50 = 21748 Funct
Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.
365 6 0 6 2.8 C1CN(CCN1CCCOC2=CC3=C(C=C2)C(=O)C=CO3)C4=CC=CC=N4
CHEMBL134746 drd1_rat Rat No 6.7 IC50 = 220 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
353 2 0 1 4.2 C1CC2CC3=CC=CC=C3CC2N(C1)CC=CI
CHEMBL39483 drd1_rat Rat No 5.7 IC50 = 2200 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
305 6 0 1 5.5 C1CC(CN(C1)CCCC2=CC=CC=C2)C=CC3=CC=CC=C3
CHEMBL70609 drd1_rat Rat No 4.7 IC50 = 22000 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
386 3 1 7 2.1 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)OS(=O)(=O)C
CHEMBL13588 drd1_rat Rat No 5.7 IC50 = 2210 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
338 2 2 3 1.5 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CN5CC(=O)NC5=O
CHEMBL71 drd1_human Human Yes 6.7 IC50 = 225 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
319 4 0 3 5.2 CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
CHEMBL12628 drd1_rat Rat No 7.6 IC50 = 23 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
408 4 1 7 3.7 C1CN(CCN1CCO)C2CC(C3=C2C=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)F
CHEMBL319810 drd1_rat Rat No 7.6 IC50 = 23 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
340 2 0 2 4.7 CN1CCC(=CC1)C2=CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL2057445 drd1_human Human No 4.6 IC50 = 23280 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
355 4 0 5 3.2 COC1=CC(=C2C3CC4=CC(=CC(=C4CN3CCC2=C1)OC)OC)OC
CHEMBL2057445 drd1_human Human No 4.6 IC50 = 23280 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
355 4 0 5 3.2 COC1=CC(=C2C3CC4=CC(=CC(=C4CN3CCC2=C1)OC)OC)OC
CHEMBL11265 drd1_bovin Bovine No 4.6 IC50 = 23300 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
441 6 0 5 4.0 COC1=CC=CC2=C1CC3(CCCN3CCCCN4C(=O)CC5(CCCC5)CC4=O)CO2
CHEMBL422283 drd1_bovin Bovine No 4.6 IC50 = 23400 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
455 6 0 5 4.4 COC1=CC=CC2=C1CC3(CCCCN3CCCCN4C(=O)CC5(CCCC5)CC4=O)CO2
CHEMBL53 drd1_rat Rat Yes 6.6 IC50 = 238 Funct
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL54051 drd1_rat Rat No 4.6 IC50 = 23900 Funct
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
267 2 1 3 3.1 C1CNC(C2=CC3=C(C=C21)OCO3)CC4=CC=CC=C4
CHEMBL256448 drd1_rat Rat Yes 6.6 IC50 = 240 Funct
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
285 3 3 4 2.6 COC1=C(C=C2C(NCCC2=C1)CC3=CC=C(C=C3)O)O
CHEMBL256448 drd1_rat Rat Yes 6.6 IC50 = 240 Funct
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
285 3 3 4 2.6 COC1=C(C=C2C(NCCC2=C1)CC3=CC=C(C=C3)O)O
CHEMBL299471 drd1_rat Rat No 5.6 IC50 = 2400 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
397 9 0 5 3.6 CCC(=O)OC1(CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F)C3=CC=CC=C3
CHEMBL564 drd1_human Human Yes 5.6 IC50 = 2464 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
284 4 0 3 4.5 CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31
CHEMBL564 drd1_human Human Yes 5.6 IC50 = 2464 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
284 4 0 3 4.5 CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31
CHEMBL487388 drd1_rat Rat Yes 5.6 IC50 = 2500 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 2 3 5 2.3 COC1=C(C=C2CC3C4=C(C2=C1)C(=C(C=C4CCN3)O)OC)O
CHEMBL487388 drd1_rat Rat Yes 5.6 IC50 = 2500 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 2 3 5 2.3 COC1=C(C=C2CC3C4=C(C2=C1)C(=C(C=C4CCN3)O)OC)O
CHEMBL114280 drd1_human Human No 5.6 IC50 = 2500 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
360 6 2 4 2.6 C1OC2=C(O1)C=C(C(=C2)CNCCCN3C4=CC=CC=C4NC3=O)Cl
CHEMBL1275791 drd1_human Human No 4.6 IC50 = 25000 Funct
Binding affinity to dopamine D1Binding affinity to dopamine D1
246 2 1 2 3.2 CN(C)C1CCC(C1)C2=CNC3=C2C=C(C=C3)F
CHEMBL1275791 drd1_human Human No 4.6 IC50 = 25000 Funct
Binding affinity to dopamine D1Binding affinity to dopamine D1
246 2 1 2 3.2 CN(C)C1CCC(C1)C2=CNC3=C2C=C(C=C3)F
CHEMBL1306 drd1_human Human Yes 4.6 IC50 = 25480 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL1306 drd1_human Human Yes 4.6 IC50 = 25480 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
532 8 0 7 4.8 CC(C)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=NC=N4)C5=C(C=C(C=C5)Cl)Cl
CHEMBL292006 drd1_rat Rat No 5.6 IC50 = 2600 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
412 9 0 5 4.6 CCC(=O)OC1(CCN(CC1C)CCCC(=O)C2=CC=C(C=C2)F)C3=CC=CC=C3
CHEMBL57140 drd1_rat Rat No 5.6 IC50 = 2650 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
355 6 1 4 3.6 CC1CN(CCC1(C2=CC=CC=C2)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL421914 drd1_rat Rat No 6.6 IC50 = 270 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
383 3 0 2 4.1 COC1=CC=CC2=C1CCC3C2CCCN3CC=CI
CHEMBL49 drd1_bovin Bovine Yes 4.6 IC50 = 27000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
386 6 0 6 2.6 C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4
CHEMBL114484 drd1_human Human No 5.6 IC50 = 2740 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
356 3 1 2 4.5 CC1=CC(=C(C=C1)CN2CCC(CC2)N3C4=CC=CC=C4NC3=O)Cl
CHEMBL643 drd1_human Human Yes 5.6 IC50 = 2744 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
284 3 0 3 4.8 CC(CN1C2=CC=CC=C2SC3=CC=CC=C31)N(C)C
CHEMBL117537 drd1_human Human No 5.6 IC50 = 2750 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
477 10 0 4 6.1 C1CN(CCN1CCCC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)CCCC4=CC=CC=C4
CHEMBL1381098 drd1_human Human Yes 4.6 IC50 = 27576 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
185 1 0 2 4.3 C1=CC=C2C(=C1)C=CC=C2N=C=S
CHEMBL1381098 drd1_human Human Yes 4.6 IC50 = 27576 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
185 1 0 2 4.3 C1=CC=C2C(=C1)C=CC=C2N=C=S
CHEMBL18797 drd1_human Human Yes 4.6 IC50 = 27822 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
340 4 1 4 4.8 CC1=C(C2=C(C1=CC3=CC=C(C=C3)SC)C=CC(=C2)F)CC(=O)O
CHEMBL118 drd1_human Human Yes 4.6 IC50 = 27994 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
381 3 1 7 3.4 CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
CHEMBL118 drd1_human Human Yes 4.6 IC50 = 27994 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
381 3 1 7 3.4 CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
CHEMBL286120 drd1_rat Rat No 5.6 IC50 = 2800 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
295 3 2 3 3.6 C=CCN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O
CHEMBL54206 drd1_rat Rat Yes 5.6 IC50 = 2800 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
341 6 1 4 2.6 C1CN(CCC1(C2=CC=CC=C2)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL85879 drd1_rat Rat No 5.6 IC50 = 2820 Funct
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
294 6 0 2 4.5 C1CN(CCN1CCCCC2=CC=CC=C2)C3=CC=CC=C3
CHEMBL320481 drd1_rat Rat No 5.5 IC50 = 2900 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
251 0 2 2 2.9 C1CC2=C(C=CC=C2O)C3C1NCC4=CC=CC=C34
CHEMBL1909065 drd1_human Human No 5.5 IC50 = 2908 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
917 13 4 17 3.9 CC1CC(C(OC1C2CC(C(O2)C3(CCC(O3)C4(CCC5(O4)CC(C(C(O5)C(C)C6C(C(C(C(O6)(CC(=O)O)O)C)OC)OC)C)O)C)C)OC7CC(C(C(O7)C)OC)OC)(C)O)C
CHEMBL1909065 drd1_human Human No 5.5 IC50 = 2908 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
917 13 4 17 3.9 CC1CC(C(OC1C2CC(C(O2)C3(CCC(O3)C4(CCC5(O4)CC(C(C(O5)C(C)C6C(C(C(C(O6)(CC(=O)O)O)C)OC)OC)C)O)C)C)OC7CC(C(C(O7)C)OC)OC)(C)O)C
CHEMBL2057452 drd1_human Human No 5.5 IC50 = 2917.2 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL2057452 drd1_human Human No 5.5 IC50 = 2917.2 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL292274 drd1_rat Rat No 4.5 IC50 = 29200 Funct
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
214 1 1 1 2.8 CN(C)C1CCC2=C(C1)C3=C(C=C2)NC=C3
CHEMBL256075 drd1_rat Rat Yes 8.5 IC50 = 3 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
453 2 2 5 3.4 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)I
CHEMBL256075 drd1_rat Rat Yes 8.5 IC50 = 3 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
453 2 2 5 3.4 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)I
CHEMBL137536 drd1_rat Rat No 8.4 IC50 = 3.8 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
356 2 0 4 4.3 CC1(CN(CCN1C)C2CC(C3=C2C(=CC=C3)F)C4=CC=C(C=C4)F)C
CHEMBL2057456 drd1_human Human No 7.5 IC50 = 30.7 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
371 4 2 6 2.0 COC1=CC(=C(C2=C1CN3CCC4=CC(=C(C=C4C3C2)O)OC)CO)OC
CHEMBL112037 drd1_rat Rat No 5.5 IC50 = 3000 Funct
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
330 5 0 2 5.4 C1CN(CCN1CCCC2=CC3=CC=CC=C3C=C2)C4=CC=CC=C4
CHEMBL53 drd1_rat Rat Yes 5.5 IC50 = 3000 Funct
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL141863 drd1_rat Rat No 5.5 IC50 = 3000 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
307 2 0 2 5.1 CCN1CCC2=C(C(C1)C3=CC=CC=C3)SC4=CC=CC=C24
CHEMBL26018 drd1_bovin Bovine No 4.5 IC50 = 30000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
447 11 1 6 4.6 CCCN(CCCCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL300735 drd1_bovin Bovine No 4.5 IC50 = 30000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
447 11 1 6 4.6 CCCN(CCCCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL308843 drd1_rat Rat No 6.5 IC50 = 305 Funct
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
351 1 0 2 5.0 CC=C1C2=C(C=C(C=C2)Cl)C(=CC3=CC=CC=C31)N4CCN(CC4)C
CHEMBL106886 drd1_rat Rat No 5.5 IC50 = 3100 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
325 2 0 4 4.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C5=C(C=C4)OCO5
CHEMBL1909072 drd1_human Human Yes 7.5 IC50 = 32 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL136334 drd1_rat Rat No 7.5 IC50 = 32 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C(=CC=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL1909072 drd1_human Human Yes 7.5 IC50 = 32 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
402 5 1 4 4.4 C1CN(CCC1C(=O)N)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
CHEMBL40031 drd1_rat Rat No 6.5 IC50 = 320 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
255 4 0 1 4.6 CC(=CCN1CCCC(C1)C=CC2=CC=CC=C2)C
CHEMBL56547 drd1_rat Rat No 5.5 IC50 = 3200 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
412 9 0 5 4.6 CCC(=O)OC1(CCN(CC1C)CCCC(=O)C2=CC=C(C=C2)F)C3=CC=CC=C3
CHEMBL68680 drd1_rat Rat No 6.5 IC50 = 322 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
344 0 1 2 4.0 CN1CC2=CC=CC=C2C3C1CCC4=CC(=C(C=C34)O)Br
CHEMBL2057438 drd1_human Human No 6.5 IC50 = 323.8 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
369 3 1 6 2.2 COC1=CC(=C(C2=C1CN3CCC4=CC5=C(C=C4C3C2)OCO5)CO)OC
CHEMBL2057438 drd1_human Human No 6.5 IC50 = 323.8 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
369 3 1 6 2.2 COC1=CC(=C(C2=C1CN3CCC4=CC5=C(C=C4C3C2)OCO5)CO)OC
CHEMBL582945 drd1_human Human No 4.5 IC50 = 32700 Funct
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
625 12 2 8 5.7 CC1=CC=CC(=C1)C2CN(CCC3=CC(=C(C=C23)O)O)CCCCC4=CN(N=N4)CCCN5CCN(CC5)C6=CC=CC=C6OC
CHEMBL582945 drd1_human Human No 4.5 IC50 = 32700 Funct
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
625 12 2 8 5.7 CC1=CC=CC(=C1)C2CN(CCC3=CC(=C(C=C23)O)O)CCCCC4=CN(N=N4)CCCN5CCN(CC5)C6=CC=CC=C6OC
CHEMBL117841 drd1_rat Rat No 5.5 IC50 = 3276 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
265 1 0 2 3.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC
CHEMBL512542 drd1_rat Rat No 4.5 IC50 = 32900 Funct
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
299 4 2 4 2.9 COC1=CC=C(C=C1)CC2C3=CC(=C(C=C3CCN2)O)OC
CHEMBL512542 drd1_rat Rat No 4.5 IC50 = 32900 Funct
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
299 4 2 4 2.9 COC1=CC=C(C=C1)CC2C3=CC(=C(C=C3CCN2)O)OC
CHEMBL124561 drd1_rat Rat Yes 7.5 IC50 = 33 Funct
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
253 0 3 3 2.1 C1C2C3=C(CC4=C2C(=CC=C4)CN1)C(=C(C=C3)O)O
CHEMBL53294 drd1_rat Rat Yes 5.5 IC50 = 3300 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
325 3 2 4 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O
CHEMBL11425 drd1_human Human No 5.5 IC50 = 3311.3 Funct
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
385 7 1 4 3.4 C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCNCC3CC4=CC=CC=C4OC3
CHEMBL53294 drd1_rat Rat Yes 5.5 IC50 = 3340 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
325 3 2 4 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O
CHEMBL345822 drd1_rat Rat No 5.5 IC50 = 3340 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)Br)O
CHEMBL54 drd1_rat Rat Yes 6.5 IC50 = 337 Funct
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL139258 drd1_rat Rat No 7.5 IC50 = 34 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
389 2 0 2 5.3 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)Cl)C
CHEMBL273526 drd1_rat Rat No 5.5 IC50 = 3430 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
416 4 2 2 5.3 CC(C)(C)C1=CC2=C3C(=CN2)CC4C(C3=C1)CC(CN4C)CNC(=O)C5=CC=CC=C5
CHEMBL11262 drd1_human Human No 4.5 IC50 = 34673.7 Funct
Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.
277 7 0 3 4.0 CCCN(CCC)CC1CC2=C(C=CC=C2OC)OC1
CHEMBL24077 drd1_rat Rat Yes 7.5 IC50 = 35 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL13464 drd1_rat Rat No 5.5 IC50 = 3540 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
395 3 2 3 3.2 CC(C)(C)C1=C2C3=C(C=C1)C4CC(CN(C4CC3=CN2)C)CN5CC(=O)NC5=O
CHEMBL54 drd1_rat Rat Yes 7.4 IC50 = 36 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL54 drd1_rat Rat Yes 7.4 IC50 = 36 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL257746 drd1_rat Rat Yes 4.4 IC50 = 36000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
281 0 2 4 2.5 C1CNC2CC3=C(C=CC(=C3)O)C4=C2C1=CC5=C4OCO5
CHEMBL257746 drd1_rat Rat Yes 4.4 IC50 = 36000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
281 0 2 4 2.5 C1CNC2CC3=C(C=CC(=C3)O)C4=C2C1=CC5=C4OCO5
CHEMBL416288 drd1_rat Rat Yes 5.4 IC50 = 3620 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
267 0 2 3 2.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O
CHEMBL136891 drd1_rat Rat No 7.4 IC50 = 37 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=CC(=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL21731 drd1_human Human Yes 6.4 IC50 = 373 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
277 4 1 1 4.6 CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24
CHEMBL21731 drd1_human Human Yes 6.4 IC50 = 373 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
277 4 1 1 4.6 CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24
CHEMBL116463 drd1_human Human No 6.4 IC50 = 376 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
518 11 1 6 6.5 C1CN(CCC1NC(=O)OCCC2=CC=C(C=C2)C#N)CCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL136480 drd1_rat Rat No 7.4 IC50 = 38 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
324 2 0 3 3.9 CC1=CC2=C(C=C1)C(CC2N3CCN(CC3)C)C4=CC=C(C=C4)F
CHEMBL137486 drd1_bovin Bovine No 4.4 IC50 = 38000 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
459 8 1 6 4.4 CC1=CC=C(C=C1)S(=O)(=O)NCCCCN2CCCCC23CC4=C(C=CC=C4OC)OC3
CHEMBL13770 drd1_rat Rat No 5.4 IC50 = 3810 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
438 3 2 4 4.1 CC(C)(C)C1=CC2=C3C(=CN2)CC4C(C3=C1)CC(CN4C)C(=O)NC5=NN=C(C=C5)Cl
CHEMBL334498 drd1_bovin Bovine No 4.4 IC50 = 38300 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
427 7 1 5 4.5 COC1=CC=CC2=C1CC3(CCCCN3CCCCNC(=O)C4=CC=C(C=C4)F)CO2
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 384 Funct
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 384 Funct
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 384 Funct
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 384 Funct
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL81 drd1_human Human Yes 5.4 IC50 = 3864 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
474 7 2 6 6.1 C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O
CHEMBL81 drd1_human Human Yes 5.4 IC50 = 3864 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
474 7 2 6 6.1 C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O
CHEMBL30008 drd1_human Human Yes 5.4 IC50 = 3874 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
405 6 0 4 6.0 C1CN(CCN1CC=CC2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL30008 drd1_human Human Yes 5.4 IC50 = 3874 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
405 6 0 4 6.0 C1CN(CCN1CC=CC2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL337542 drd1_rat Rat No 7.4 IC50 = 39 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
387 5 1 5 3.4 CSC1=CC2=C(C=C1)C(CC2N3CCN(CC3)CCO)C4=CC=C(C=C4)F
CHEMBL1113 drd1_human Human Yes 6.4 IC50 = 392 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL1113 drd1_human Human Yes 6.4 IC50 = 392 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
314 1 1 3 2.6 C1CN(CCN1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
CHEMBL11592 drd1_human Human Yes 4.4 IC50 = 39810.7 Funct
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
443 9 0 5 4.6 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL34095 drd1_rat Rat No 8.4 IC50 = 4.3 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
374 3 2 3 4.3 C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Br
CHEMBL62 drd1_rat Rat Yes 8.4 IC50 = 4.3 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL136468 drd1_rat Rat No 8.4 IC50 = 4.4 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=CC=C4F)C
CHEMBL2057455 drd1_human Human No 8.3 IC50 = 4.9 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
341 3 1 5 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)OC
CHEMBL258370 drd1_rat Rat No 6.4 IC50 = 400 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
295 0 1 4 2.9 CN1CCC2=CC3=C(C4=C2C1CC5=C4C(=CC=C5)O)OCO3
CHEMBL388342 drd1_rat Rat Yes 6.4 IC50 = 400 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 2 5 2.7 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O
CHEMBL388342 drd1_rat Rat Yes 6.4 IC50 = 400 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
327 2 2 5 2.7 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O
CHEMBL258370 drd1_rat Rat No 6.4 IC50 = 400 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
295 0 1 4 2.9 CN1CCC2=CC3=C(C4=C2C1CC5=C4C(=CC=C5)O)OCO3
CHEMBL388342 drd1_rat Rat Yes 6.4 IC50 = 400 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 2 5 2.7 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O
CHEMBL388342 drd1_rat Rat Yes 6.4 IC50 = 400 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
327 2 2 5 2.7 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O
CHEMBL12028 drd1_rat Rat No 6.4 IC50 = 400 Funct
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
460 7 1 8 3.8 CC1=C(SC2=C1C(=O)N(C(=N2)SCCCN3CCN(CC3)C4=CC=CC=C4OC)N)C
CHEMBL283207 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
423 9 0 5 4.3 CCCN(CCCCN1C(=O)C2=CC=CC=C2C1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL52396 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
423 9 0 5 4.3 CCCN(CCCCN1C(=O)C2=CC=CC=C2C1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL26783 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
413 8 0 4 4.6 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=CC=CC=C4OC3
CHEMBL50993 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
413 8 0 4 4.6 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=CC=CC=C4OC3
CHEMBL423841 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
408 8 0 5 3.9 CCCN(CCCN1C(=O)C2=CC=CC=C2C1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL54089 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
408 8 0 5 3.9 CCCN(CCCN1C(=O)C2=CC=CC=C2C1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL52438 drd1_bovin Bovine No 4.4 IC50 = 40000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
283 5 0 2 5.1 CCCN(CCC)C1CC2=C(C=CC3=CC=CC=C23)OC1
CHEMBL11592 drd1_bovin Bovine Yes 4.4 IC50 = 40000 Funct
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
443 9 0 5 4.6 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C3CC4=C(C=CC=C4OC)OC3
CHEMBL296419 drd1_human Human Yes 5.4 IC50 = 4010 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
459 8 1 5 6.0 COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
CHEMBL296419 drd1_human Human Yes 5.4 IC50 = 4010 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
459 8 1 5 6.0 COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
CHEMBL1403281 drd1_human Human Yes 6.4 IC50 = 403 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
576 5 3 6 2.7 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=CNC7=CC=CC(=C67)C5=C4)C)O
CHEMBL1262 drd1_human Human Yes 5.4 IC50 = 4136.1 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
429 6 0 3 6.1 C1=CC(=C(C=C1Cl)Cl)CON=C(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl
CHEMBL14048 drd1_rat Rat No 5.4 IC50 = 4150 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
359 3 2 2 3.6 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CNC(=O)C5=CC=CC=C5
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 430 Funct
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 432 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL13866 drd1_rat Rat Yes 5.4 IC50 = 4340 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
240 0 1 1 3.2 CC1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)C
CHEMBL343282 drd1_rat Rat No 6.4 IC50 = 440 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
347 2 1 3 3.9 CC1(CN(CCN1)C2CC(C3=C2C=C(C=C3)Cl)C4=CSC=C4)C
CHEMBL270299 drd1_human Human Yes 5.4 IC50 = 4412 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
249 3 0 3 2.7 CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N
CHEMBL270299 drd1_human Human Yes 5.4 IC50 = 4412 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
249 3 0 3 2.7 CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N
CHEMBL328246 drd1_rat Rat No 6.4 IC50 = 443 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
365 1 0 2 5.6 CC(=C1C2=C(C=C(C=C2)Cl)C=C(C3=CC=CC=C31)N4CCN(CC4)C)C
CHEMBL53 drd1_rat Rat Yes 6.4 IC50 = 444 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL138964 drd1_rat Rat No 7.4 IC50 = 45 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=CC=C3Cl)C4=CC=C(C=C4)F)C
CHEMBL2057446 drd1_human Human No 7.3 IC50 = 45.5 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
385 5 0 6 3.2 COC1=CC(=C2CN3CCC4=CC(=C(C(=C4C3CC2=C1)OC)OC)OC)OC
CHEMBL170475 drd1_rat Rat No 6.4 IC50 = 450 Funct
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
307 3 0 2 4.5 COC1=CC=CC2=C1CC3CCCN(C3C2)CC4=CC=CC=C4
CHEMBL14020 drd1_rat Rat No 5.3 IC50 = 4580 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
413 3 3 3 4.4 CC(=O)NC(=S)NCC1CC2C(CC3=CNC4=C(C=CC2=C34)C(C)(C)C)N(C1)C
CHEMBL611207 drd1_human Human No 6.3 IC50 = 460 Funct
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
387 4 0 5 4.5 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C
CHEMBL611207 drd1_human Human No 6.3 IC50 = 460 Funct
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
387 4 0 5 4.5 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C
CHEMBL85 drd1_human Human Yes 6.3 IC50 = 479 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
411 4 0 6 2.7 CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL85 drd1_human Human Yes 6.3 IC50 = 479 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
411 4 0 6 2.7 CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
CHEMBL343820 drd1_rat Rat No 6.3 IC50 = 480 Funct
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
292 2 0 2 3.4 CN1CCN(CC1)C2CC(C3=CC=CC=C23)C4=CC=CC=C4
CHEMBL257745 drd1_rat Rat Yes 5.3 IC50 = 4800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
295 1 1 4 2.8 COC1=C2CCNC3C2=C(C4=CC=CC=C4C3)C5=C1OCO5
CHEMBL257745 drd1_rat Rat Yes 5.3 IC50 = 4800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
295 1 1 4 2.8 COC1=C2CCNC3C2=C(C4=CC=CC=C4C3)C5=C1OCO5
CHEMBL584554 drd1_human Human No 5.3 IC50 = 4900 Funct
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
429 4 2 2 3.8 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C(=O)NC5=CC=CC=C5
CHEMBL584554 drd1_human Human No 5.3 IC50 = 4900 Funct
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
429 4 2 2 3.8 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C(=O)NC5=CC=CC=C5
CHEMBL343569 drd1_rat Rat Yes 6.3 IC50 = 491 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
297 3 0 3 3.7 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)OC)OC
CHEMBL307717 drd1_rat Rat No 8.3 IC50 = 5.3 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
328 2 0 4 3.6 CN1CCN(CC1)C2CC(C3=C2C=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL140032 drd1_rat Rat No 8.2 IC50 = 5.9 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
338 2 1 3 4.1 CC1=CC2=C(C=C1)C(CC2N3CCNC(C3)(C)C)C4=CC=C(C=C4)F
CHEMBL24077 drd1_rat Rat Yes 7.3 IC50 = 50 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL139081 drd1_rat Rat No 5.3 IC50 = 5000 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
386 2 0 2 5.8 CCN1CCC2=C(C(C1)C3=CC(=CC=C3)Br)SC4=CC=CC=C24
CHEMBL341805 drd1_rat Rat No 5.3 IC50 = 5000 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
352 2 0 4 5.0 CCN1CCC2=C(C(C1)C3=CC(=CC=C3)[N+](=O)[O-])SC4=CC=CC=C24
CHEMBL510777 drd1_rat Rat No 4.3 IC50 = 50000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 1 5 3.0 CN1CCC2=C3C1CC4=C(C(=C(C=C4)OC)O)OC3=C(C=C2)OC
CHEMBL280608 drd1_bovin Bovine No 4.3 IC50 = 50000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
419 9 1 6 3.9 CCCN(CCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL51888 drd1_bovin Bovine No 4.3 IC50 = 50000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
419 9 1 6 3.9 CCCN(CCNS(=O)(=O)C1=CC=C(C=C1)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL510777 drd1_rat Rat No 4.3 IC50 = 50000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 1 5 3.0 CN1CCC2=C3C1CC4=C(C(=C(C=C4)OC)O)OC3=C(C=C2)OC
CHEMBL157879 drd1_rat Rat No 5.3 IC50 = 5061 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
251 0 1 2 2.7 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O
CHEMBL355107 drd1_rat Rat No 7.3 IC50 = 51 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
337 1 0 2 4.7 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=C)C4=CC=CC=C42
CHEMBL137954 drd1_rat Rat No 7.3 IC50 = 51 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
354 4 1 4 3.2 CC1=CC2=C(C=C1)C(CC2N3CCN(CC3)CCO)C4=CC=C(C=C4)F
CHEMBL53520 drd1_rat Rat No 4.3 IC50 = 51900 Funct
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
309 4 0 3 4.5 CCCN1CCC2=CC3=C(C=C2C1CC4=CC=CC=C4)OCO3
CHEMBL136260 drd1_rat Rat No 7.3 IC50 = 52 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
401 3 0 3 5.6 CC(C)N1CCN(CC1(C)C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL62 drd1_human Human Yes 6.3 IC50 = 520 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 6.3 IC50 = 520 Funct
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL321040 drd1_rat Rat No 6.3 IC50 = 529 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
293 2 1 2 4.2 CCCN1CC2=CC=CC=C2C3C1CCC4=C3C=C(C=C4)O
CHEMBL123642 drd1_rat Rat No 5.3 IC50 = 5300 Funct
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
253 0 3 3 2.1 C1C2C3=C(CC4=C2C(=CC=C4)CN1)C(=C(C=C3)O)O
CHEMBL445 drd1_human Human Yes 6.3 IC50 = 539 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
263 3 1 1 4.5 CNCCC=C1C2=CC=CC=C2CCC3=CC=CC=C31
CHEMBL73082 drd1_rat Rat No 6.3 IC50 = 540 Funct
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
365 1 0 2 5.6 CC(=C1C2=C(C=C(C=C2)Cl)C(=CC3=CC=CC=C31)N4CCN(CC4)C)C
CHEMBL88870 drd1_rat Rat No 6.3 IC50 = 540 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
330 1 0 2 5.0 CC(=C1C2=CC=CC=C2C=C(C3=CC=CC=C31)N4CCN(CC4)C)C
CHEMBL308090 drd1_rat Rat Yes 6.3 IC50 = 550 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
308 1 2 4 2.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)O
CHEMBL72794 drd1_rat Rat No 6.3 IC50 = 550 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
322 2 1 4 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)OC
CHEMBL308090 drd1_rat Rat Yes 6.3 IC50 = 550 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
308 1 2 4 2.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)O
CHEMBL72794 drd1_rat Rat No 6.3 IC50 = 550 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
322 2 1 4 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)OC
CHEMBL54 drd1_rat Rat Yes 6.3 IC50 = 550 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
376 6 1 4 3.2 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL113053 drd1_rat Rat No 5.3 IC50 = 5550 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
251 0 2 2 2.9 C1CC2=C(C=CC=C2O)C3C1NCC4=CC=CC=C34
CHEMBL2057457 drd1_human Human No 7.3 IC50 = 56.4 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
309 1 1 3 3.7 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)C
CHEMBL2057457 drd1_human Human No 7.3 IC50 = 56.4 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
309 1 1 3 3.7 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)C
CHEMBL153960 drd1_rat Rat No 6.3 IC50 = 561 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
286 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C(C=CC(=C43)O)Cl
CHEMBL1289 drd1_human Human Yes 6.3 IC50 = 563 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
361 2 0 1 4.6 C1=C(C(=CC(=C1Cl)Cl)Cl)OCC#CI
CHEMBL13979 drd1_rat Rat No 6.2 IC50 = 570 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
382 2 2 4 2.4 CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)C(=O)NC5=NN=C(C=C5)Cl
CHEMBL39818 drd1_rat Rat No 5.2 IC50 = 5840 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
319 7 0 1 5.8 C1CC(CN(C1)CCCCC2=CC=CC=C2)C=CC3=CC=CC=C3
CHEMBL119443 drd1_human Human Yes 5.2 IC50 = 5901 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
325 3 3 3 1.8 CC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C
CHEMBL119443 drd1_human Human Yes 5.2 IC50 = 5901 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
325 3 3 3 1.8 CC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C
CHEMBL344426 drd1_rat Rat No 8.2 IC50 = 6 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
413 2 0 3 5.8 CN1CCN(CC12CCCCC2)C3CC(C4=C3C=C(C=C4)Cl)C5=CC=C(C=C5)F
CHEMBL452776 drd1_rat Rat Yes 7.2 IC50 = 60 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)O)OC
CHEMBL452776 drd1_rat Rat Yes 7.2 IC50 = 60 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 2.7 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)O)OC
CHEMBL3344458 drd1_human Human No 6.2 IC50 = 600 Funct
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
343 4 1 4 4.4 CCCCC1=CC2=C(S1)CC3C4=CC(=C(C=C4CCN3C2)OC)O
CHEMBL3344458 drd1_human Human No 6.2 IC50 = 600 Funct
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
343 4 1 4 4.4 CCCCC1=CC2=C(S1)CC3C4=CC(=C(C=C4CCN3C2)OC)O
CHEMBL12177 drd1_rat Rat No 6.2 IC50 = 600 Funct
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
432 6 1 9 2.5 CC1=C(SC2=C1C(=O)N(C(=N2)SCCCN3CCN(CC3)C4=NC=CC=N4)N)C
CHEMBL3408841 drd1_human Human No 5.2 IC50 = 6000 Funct
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
614 10 3 8 5.4 CCOC1=C(C=CC(=N1)NC(=O)C(C)(C)NC(=O)C2=CC3=C(C=C2)C(=C(N3C)C4=NC=C(C=C4)F)C5CCCC5)C=CC(=O)O
CHEMBL3408841 drd1_human Human No 5.2 IC50 = 6000 Funct
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
614 10 3 8 5.4 CCOC1=C(C=CC(=N1)NC(=O)C(C)(C)NC(=O)C2=CC3=C(C=C2)C(=C(N3C)C4=NC=C(C=C4)F)C5CCCC5)C=CC(=O)O
CHEMBL136630 drd1_rat Rat No 6.2 IC50 = 620 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)C
CHEMBL91 drd1_human Human Yes 5.2 IC50 = 6247 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
416 6 0 2 5.3 C1=CC(=C(C=C1Cl)Cl)COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl
CHEMBL415300 drd1_rat Rat Yes 7.2 IC50 = 63 Funct
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
327 1 1 3 3.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)Cl
CHEMBL415300 drd1_rat Rat Yes 7.2 IC50 = 63 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
327 1 1 3 3.1 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)Cl
CHEMBL36979 drd1_rat Rat No 6.2 IC50 = 630 Funct
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
291 5 0 1 5.1 C1CC(CN(C1)CCC2=CC=CC=C2)C=CC3=CC=CC=C3
CHEMBL257957 drd1_rat Rat No 4.2 IC50 = 63000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 2 5 2.2 CN1CCC2=CC(=C(C3=C2C1CC4=C3C(=C(C=C4)O)O)OC)OC
CHEMBL257957 drd1_rat Rat No 4.2 IC50 = 63000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 2 5 2.2 CN1CCC2=CC(=C(C3=C2C1CC4=C3C(=C(C=C4)O)O)OC)OC
CHEMBL345907 drd1_rat Rat No 6.2 IC50 = 637 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
286 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)Cl)O
CHEMBL72292 drd1_rat Rat Yes 7.2 IC50 = 64 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
440 3 1 9 3.2 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL72292 drd1_rat Rat Yes 7.2 IC50 = 64 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
440 3 1 9 3.2 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=C2C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL225230 drd1_rat Rat Yes 6.2 IC50 = 640 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
295 2 2 3 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL299161 drd1_rat Rat No 6.2 IC50 = 651 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
309 2 2 3 3.9 CCCN1CC2=CC=CC=C2C3C1CCC4=CC(=C(C=C34)O)O
CHEMBL225853 drd1_rat Rat Yes 7.2 IC50 = 66 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
406 2 2 5 3.4 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Br
CHEMBL136262 drd1_rat Rat No 7.2 IC50 = 66 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
383 5 1 4 4.0 CC(C)C1=CC2=C(C=C1)C(CC2N3CCN(CC3)CCO)C4=CC=C(C=C4)F
CHEMBL430798 drd1_rat Rat Yes 7.2 IC50 = 66 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
441 3 0 9 3.2 CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL225853 drd1_rat Rat Yes 7.2 IC50 = 66 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
406 2 2 5 3.4 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Br
CHEMBL276175 drd1_rat Rat Yes 5.2 IC50 = 6600 Funct
compound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissuecompound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissue
443 6 0 7 4.0 C1CCC2(C1)CC(=O)N(C(=O)C2)OCCCN3CCN(CC3)C4=NSC5=CC=CC=C54
CHEMBL120995 drd1_rat Rat Yes 7.2 IC50 = 67 Funct
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
253 0 3 3 2.1 C1C2C3=C(CC4=C2C(=CC=C4)CN1)C(=C(C=C3)O)O
CHEMBL2057453 drd1_human Human No 7.2 IC50 = 68.9 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
311 2 1 4 2.9 COC1=CC2=C(CN3CCC4=CC(=C(C=C4C3C2)O)OC)C=C1
CHEMBL401798 drd1_rat Rat Yes 4.2 IC50 = 68000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
265 0 1 3 2.8 C1CNC2CC3=CC=CC=C3C4=C2C1=CC5=C4OCO5
CHEMBL401798 drd1_rat Rat Yes 4.2 IC50 = 68000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
265 0 1 3 2.8 C1CNC2CC3=CC=CC=C3C4=C2C1=CC5=C4OCO5
CHEMBL2057451 drd1_human Human No 6.2 IC50 = 684 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL2057451 drd1_human Human No 6.2 IC50 = 684.0 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL73151 drd1_rat Rat Yes 7.2 IC50 = 69 Funct
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
340 3 2 2 2.5 CCN(CC)C(=O)NC1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)C
CHEMBL139304 drd1_rat Rat No 6.2 IC50 = 690 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
419 5 1 6 2.1 CS(=O)(=O)C1=CC2=C(C=C1)C(CC2N3CCN(CC3)CCO)C4=CC=C(C=C4)F
CHEMBL25856 drd1_rat Rat No 8.2 IC50 = 7.2 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL194837 drd1_human Human No 8.1 IC50 = 7.5 Funct
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
448 8 1 5 5.0 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)COC3=C(C=C(C=C3)Cl)Cl)OCCN(C)C
CHEMBL194837 drd1_human Human No 8.1 IC50 = 7.5 Funct
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
448 8 1 5 5.0 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)COC3=C(C=C(C=C3)Cl)Cl)OCCN(C)C
CHEMBL134273 drd1_rat Rat No 6.2 IC50 = 700 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
241 1 1 2 2.8 C#CCN1CCCC2C1CC3=C(C2)C(=CC=C3)O
CHEMBL250699 drd1_human Human Yes 5.2 IC50 = 7000 Funct
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
358 5 1 4 4.4 COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC
CHEMBL250699 drd1_human Human Yes 5.2 IC50 = 7000 Funct
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
358 5 1 4 4.4 COC1=CC(=CC(=C1)NC(=O)C2=CC=C(O2)C3=CC=C(C=C3)Cl)OC
CHEMBL336437 drd1_rat Rat No 4.2 IC50 = 70000 Funct
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
376 2 0 2 6.4 CCN1CCC2=C(C(C1)C3=CC(=C(C=C3)Cl)Cl)SC4=CC=CC=C24
CHEMBL715 drd1_human Human Yes 7.1 IC50 = 72 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
312 1 1 5 2.8 CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
CHEMBL1275709 drd1_human Human No 5.1 IC50 = 7200 Funct
Binding affinity to dopamine D1Binding affinity to dopamine D1
253 2 1 2 2.8 CN(C)C1CCC(C1)C2=CNC3=C2C=C(C=C3)C#N
CHEMBL1275709 drd1_human Human No 5.1 IC50 = 7200 Funct
Binding affinity to dopamine D1Binding affinity to dopamine D1
253 2 1 2 2.8 CN(C)C1CCC(C1)C2=CNC3=C2C=C(C=C3)C#N
CHEMBL14089 drd1_rat Rat No 5.1 IC50 = 7220 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
438 3 2 4 4.1 CC(C)(C)C1=C2C3=C(C=C1)C4CC(CN(C4CC3=CN2)C)C(=O)NC5=NN=C(C=C5)Cl
CHEMBL136333 drd1_rat Rat No 6.1 IC50 = 730 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
322 4 1 3 2.8 C1CN(CCN1CCO)C2CC(C3=CC=CC=C23)C4=CC=CC=C4
CHEMBL275539 drd1_rat Rat No 5.1 IC50 = 7390 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
395 3 2 3 3.2 CC(C)(C)C1=CC2=C3C(=CN2)CC4C(C3=C1)CC(CN4C)CN5CC(=O)NC5=O
CHEMBL72220 drd1_rat Rat No 7.1 IC50 = 74 Funct
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
339 1 0 2 4.9 CC1C2=C(C=C(C=C2)Cl)C(=CC3=CC=CC=C13)N4CCN(CC4)C
CHEMBL73074 drd1_rat Rat No 5.1 IC50 = 7400 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
322 2 1 5 2.6 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)OC
CHEMBL73074 drd1_rat Rat No 5.1 IC50 = 7400 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
322 2 1 5 2.6 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)OC
CHEMBL14376 drd1_mouse Mouse Yes 6.1 IC50 = 750 Funct
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
426 8 0 7 4.1 CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
CHEMBL56843 drd1_rat Rat No 5.1 IC50 = 7500 Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
325 6 0 3 4.3 C1CN(CCC1C2=CC=CC=C2)CCCC(=O)C3=CC=C(C=C3)F
CHEMBL37736 drd1_rat Rat Yes 4.1 IC50 = 75000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
275 0 0 4 3.4 C1OC2=C(O1)C3=C4C(=C2)C=CN=C4C(=O)C5=CC=CC=C53
CHEMBL37736 drd1_rat Rat Yes 4.1 IC50 = 75000 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
275 0 0 4 3.4 C1OC2=C(O1)C3=C4C(=C2)C=CN=C4C(=O)C5=CC=CC=C53
CHEMBL13811 drd1_rat Rat No 5.1 IC50 = 7530 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
296 1 1 1 4.8 CC1CC2C(CC3=CNC4=C(C=CC2=C34)C(C)(C)C)N(C1)C
CHEMBL115444 drd1_human Human No 5.1 IC50 = 7580 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
430 4 1 5 3.1 C1CN(CCC1N2C3=CC=CC=C3NC2=O)C(=O)OCC4=CC5=C(C=C4Cl)OCO5
CHEMBL411 drd1_human Human Yes 5.1 IC50 = 7763 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
268 4 2 2 5.1 CCC(=C(CC)C1=CC=C(C=C1)O)C2=CC=C(C=C2)O
CHEMBL411 drd1_human Human Yes 5.1 IC50 = 7763 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
268 4 2 2 5.1 CCC(=C(CC)C1=CC=C(C=C1)O)C2=CC=C(C=C2)O
CHEMBL72162 drd1_rat Rat No 8.1 IC50 = 8 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
337 1 0 2 4.7 CN1CCN(CC1)C2=CC3=CC=CC=C3C(=C)C4=C2C=C(C=C4)Cl
CHEMBL284473 drd1_rat Rat No 8.1 IC50 = 8.1 Funct
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
295 3 2 3 3.6 C=CCN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O
CHEMBL2334893 drd1_human Human No 8.1 IC50 = 8.2 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
325 1 1 5 2.8 COC1=C(C=C2C3CC4=CC5=C(C=C4CN3CCC2=C1)OCO5)O
CHEMBL422067 drd1_rat Rat No 8.1 IC50 = 8.3 Funct
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
375 4 1 4 3.5 C1CN(CCN1CCO)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL137805 drd1_rat Rat No 8.1 IC50 = 8.8 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
401 4 0 3 5.8 CCC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)CC
CHEMBL336274 drd1_rat Rat No 7.1 IC50 = 80 Funct
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
383 3 0 2 4.2 COC1=CC=CC2=C1CC3CCCN(C3C2)CC=CI
CHEMBL479 drd1_rat Rat Yes 7.1 IC50 = 80 Funct
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
371 4 0 4 5.9 CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)SC
CHEMBL455633 drd1_rat Rat Yes 6.1 IC50 = 800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 1 5 3.0 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)OC)OC
CHEMBL455633 drd1_rat Rat Yes 6.1 IC50 = 800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
327 2 1 5 3.0 CN1CCC2=C3C1CC4=CC(=C(C=C4OC3=C(C=C2)O)OC)OC
CHEMBL154787 drd1_rat Rat No 6.1 IC50 = 800 Funct
In vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
459 7 1 7 4.5 CC1=C(SC2=C1C(=O)N(C(=N2)SCCCN3CCC(CC3)C4=CC=CC=C4OC)N)C
CHEMBL26975 drd1_bovin Bovine No 4.1 IC50 = 80000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
417 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(CC1=O)(C)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL52485 drd1_bovin Bovine No 4.1 IC50 = 80000 Funct
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
417 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(CC1=O)(C)C)C2CC3=C(C=CC=C3OC)OC2
CHEMBL524439 drd1_rat Rat Yes 7.1 IC50 = 81 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
362 2 2 5 3.3 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Cl
CHEMBL524439 drd1_rat Rat Yes 7.1 IC50 = 81 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
362 2 2 5 3.3 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Cl
CHEMBL154989 drd1_rat Rat No 6.1 IC50 = 818 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=CC(=CC(=C43)O)Br
CHEMBL416523 drd1_human Human No 6.1 IC50 = 831.8 Funct
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
415 8 1 5 3.4 COC1=CC=CC2=C1CC(CO2)CNCCCCN3C(=O)CC4(CCCC4)CC3=O
CHEMBL87321 drd1_rat Rat No 6.1 IC50 = 849 Funct
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
288 2 2 2 3.9 CNC1CC(C2=CC(=C(C=C2C1)Cl)O)C3=CC=CC=C3
CHEMBL14022 drd1_rat Rat No 6.1 IC50 = 850 Funct
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
426 6 2 4 2.8 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)C
CHEMBL83 drd1_human Human Yes 5.1 IC50 = 8502 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
372 8 0 2 7.1 CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
CHEMBL83 drd1_human Human Yes 5.1 IC50 = 8502 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
372 8 0 2 7.1 CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
CHEMBL346017 drd1_rat Rat No 5.1 IC50 = 8611 Funct
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
330 0 1 2 3.3 CN1CCC2=CC=CC3=C2C1CC4=C(C=CC(=C43)O)Br
CHEMBL73538 drd1_rat Rat Yes 6.1 IC50 = 895 Funct
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
292 1 1 3 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=CC=CC=C42
CHEMBL73538 drd1_rat Rat Yes 6.1 IC50 = 895 Funct
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
292 1 1 3 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=CC=CC=C42
CHEMBL2111937 drd1_rat Rat No 8.0 IC50 = 9.5 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
345 2 0 3 4.2 CN1CCN(CC1)C2CC(C3=C2C=CC(=C3)Cl)C4=CC=C(C=C4)F
CHEMBL318714 drd1_rat Rat No 8.0 IC50 = 9.5 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
345 2 0 3 4.2 CN1CCN(CC1)C2CC(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL136873 drd1_rat Rat No 8.0 IC50 = 9.6 Funct
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
373 2 0 3 4.8 CC1(CN(CCN1C)C2CC(C3=C2C=C(C=C3)Cl)C4=CC(=CC=C4)F)C
CHEMBL12507 drd1_rat Rat No 8.0 IC50 = 9.8 Funct
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
341 2 0 2 4.6 CN1CCC(=CC1)C2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F
CHEMBL2057455 drd1_human Human No 8.0 IC50 = 9.9 Funct
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
341 3 1 5 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)O)OC)OC
CHEMBL189118 drd1_human Human No 6.1 IC50 = 900 Funct
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
473 8 1 8 5.5 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)C=CC3=CC=C(C=C3)OC(F)(F)F)N(C)CCN(C)C
CHEMBL189118 drd1_human Human No 6.1 IC50 = 900 Funct
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
473 8 1 8 5.5 CC1=CC(=NC2=C1C=C(C=C2)NC(=O)C=CC3=CC=C(C=C3)OC(F)(F)F)N(C)CCN(C)C
CHEMBL104 drd1_human Human Yes 5.0 IC50 = 9017 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL104 drd1_human Human Yes 5.1 IC50 = 9017 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
345 4 0 1 5.0 C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4
CHEMBL51017 drd1_rat Rat No 7.0 IC50 = 91 Funct
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
281 0 2 3 3.0 CN1CC2=CC=CC=C2C3C1CCC4=CC(=C(C=C34)O)O
CHEMBL633 drd1_human Human Yes 5.0 IC50 = 9142 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
645 11 0 4 7.6 CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I
CHEMBL633 drd1_human Human Yes 5.0 IC50 = 9142 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
645 11 0 4 7.6 CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I
CHEMBL808 drd1_human Human Yes 5.0 IC50 = 9225 Funct
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
382 6 0 2 5.3 C1=CC(=CC=C1COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl
CHEMBL310712 drd1_rat Rat No 6.0 IC50 = 930 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
440 3 1 10 3.4 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL310712 drd1_rat Rat No 6.0 IC50 = 930 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
440 3 1 10 3.4 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)OS(=O)(=O)C(F)(F)F
CHEMBL418791 drd1_rat Rat Yes 6.0 IC50 = 955 Funct
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
281 0 2 3 3.0 CN1CC2=CC=CC=C2C3C1CCC4=C3C=CC(=C4O)O
CHEMBL2047561 drd1_human Human No 5.0 IC50 = 9650 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
364 6 1 3 4.7 C1CN(CC=C1CC2=CC=CC=C2)CCC(C3=CC4=CC=CC=C4S3)O
CHEMBL2047561 drd1_human Human No 5.0 IC50 = 9650 Funct
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
364 6 1 3 4.7 C1CN(CC=C1CC2=CC=CC=C2)CCC(C3=CC4=CC=CC=C4S3)O
CHEMBL113956 drd1_human Human No 6.0 IC50 = 967 Funct
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
522 11 1 5 6.0 CCOC1=CC=C(C=C1)CCNC(=O)N2CCN(CC2)CCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
CHEMBL322574 drd1_rat Rat No 6.0 IC50 = 970 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
374 2 2 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)Br)C(=C(C=C4)O)O
CHEMBL322574 drd1_rat Rat No 6.0 IC50 = 970 Funct
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
374 2 2 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)Br)C(=C(C=C4)O)O
CHEMBL322574 drd1_rat Rat No 6.0 IC50 = 970 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
374 2 2 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)Br)C(=C(C=C4)O)O
CHEMBL2057454 drd1_human Human No 7.0 IC50 = 98.1 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
371 4 1 6 2.9 COC1=CC(=C2CN3CCC4=CC(=C(C(=C4C3CC2=C1)OC)O)OC)OC
CHEMBL508011 drd1_rat Rat Yes 5.0 IC50 = 9800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
297 2 2 4 2.6 COC1=C2CCNC3C2=C(C4=CC=CC=C4C3)C(=C1OC)O
CHEMBL70377 drd1_rat Rat Yes 5.0 IC50 = 9800 Funct
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
308 1 2 5 2.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)O
CHEMBL508011 drd1_rat Rat Yes 5.0 IC50 = 9800 Funct
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
297 2 2 4 2.6 COC1=C2CCNC3C2=C(C4=CC=CC=C4C3)C(=C1OC)O
CHEMBL70377 drd1_rat Rat Yes 5.0 IC50 = 9800 Funct
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
308 1 2 5 2.2 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)O
CHEMBL434215 drd1_human Human Yes 9.8 Kd = 0.2 Funct
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
420 2 1 4 4.9 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)N=[N+]=[N-])O)I
CHEMBL150800 drd1_human Human No 9.6 Kd = 0.3 Funct
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
420 2 1 4 4.9 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)N=[N+]=[N-])O)I
CHEMBL1185 drd1_rat Rat Yes 9.5 Kd = 0.3 Funct
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
287 5 2 3 2.2 CN(C)CCC1=CNC2=C1C=C(C=C2)CC3COC(=O)N3
CHEMBL62 drd1_human Human Yes 9.4 Kd = 0.4 Funct
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL2114388 drd1_rat Rat No 8.9 Kd = 1.4 Funct
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
412 1 1 2 4.6 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)I)O)Cl
CHEMBL3423404 drd1_human Human No 5.9 Kd = 1200 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
674 16 7 7 3.0 CCCCC(C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CCCCN)C(=O)N)NC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL226639 drd1_human Human No 5.9 Kd = 1200 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
631 10 4 5 4.5 CC(C)C(C(=O)N1CCCC1C(=O)N)NC(=O)C(CCC2CCCCC2)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL3423404 drd1_human Human No 5.9 Kd = 1200 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
674 16 7 7 3.0 CCCCC(C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CCCCN)C(=O)N)NC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL226639 drd1_human Human No 5.9 Kd = 1200 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
631 10 4 5 4.5 CC(C)C(C(=O)N1CCCC1C(=O)N)NC(=O)C(CCC2CCCCC2)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL3423407 drd1_human Human No 5.9 Kd = 1300 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
694 16 6 8 3.6 CCCCC(C(=O)NC(CC1=CC(=C(C=C1)F)F)C(=O)NC(CCCCN)C(=O)N)NC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL3423407 drd1_human Human No 5.9 Kd = 1300 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
694 16 6 8 3.6 CCCCC(C(=O)NC(CC1=CC(=C(C=C1)F)F)C(=O)NC(CCCCN)C(=O)N)NC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL24077 drd1_human Human Yes 6.8 Kd = 150 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
255 1 3 3 2.5 C1CNCC(C2=CC(=C(C=C21)O)O)C3=CC=CC=C3
CHEMBL3423410 drd1_human Human No 5.8 Kd = 1500 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423410 drd1_human Human No 5.8 Kd = 1500 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423403 drd1_human Human No 4.8 Kd = 15000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423403 drd1_human Human No 4.8 Kd = 15000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423411 drd1_human Human No 5.8 Kd = 1600 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423411 drd1_human Human No 5.8 Kd = 1600 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL225230 drd1_human Human Yes 5.7 Kd = 1816 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
295 2 2 3 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL1161520 drd1_human Human Yes 5.7 Kd = 1818 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
306 1 3 3 3.0 C1C[NH2+]CC(C2=CC(=C(C(=C21)Cl)[O-])O)C3=CC=C(C=C3)O
CHEMBL3423406 drd1_human Human No 5.7 Kd = 1900 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
697 16 7 6 3.5 CCCCC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CCCCN)C(=O)N)NC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL3423406 drd1_human Human No 5.7 Kd = 1900 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
697 16 7 6 3.5 CCCCC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CCCCN)C(=O)N)NC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL287504 drd1_rat Rat Yes 6.7 Kd = 197 Funct
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
253 1 1 2 3.4 CN1CCC2=C(C=C(C=C2)O)C(C1)C3=CC=CC=C3
CHEMBL416401 drd1_rat Rat No 8.6 Kd = 2.3 Funct
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
332 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br
CHEMBL3423410 drd1_human Human No 4.6 Kd = 24000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423410 drd1_human Human No 4.6 Kd = 24000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423400 drd1_human Human No 4.6 Kd = 27000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
660 11 5 7 2.8 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CC(CC2C(=O)N)N)NC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL3423400 drd1_human Human No 4.6 Kd = 27000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
660 11 5 7 2.8 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CC(CC2C(=O)N)N)NC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL3423402 drd1_human Human No 5.5 Kd = 2900 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
794 18 7 7 2.7 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CNC7=CC=CC=C76)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423402 drd1_human Human No 5.5 Kd = 2900 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
794 18 7 7 2.7 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CNC7=CC=CC=C76)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423411 drd1_human Human No 4.5 Kd = 30000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423411 drd1_human Human No 4.5 Kd = 30000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
791 18 6 9 2.8 C1CC(N(C1)C(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4)C(=O)NC(CC6=CC(=C(C=C6)F)F)C(=O)NC(CCCCN)C(=O)N
CHEMBL3423409 drd1_human Human No 5.5 Kd = 3300 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
789 22 7 8 3.8 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)NC(CCCCN)C(=O)N)NC(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL3423409 drd1_human Human No 5.5 Kd = 3300 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
789 22 7 8 3.8 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)NC(CCCCN)C(=O)N)NC(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL3423405 drd1_human Human No 5.5 Kd = 3400 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
794 17 7 7 3.1 CCCCC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CC(CC3C(=O)N)N)NC(=O)CCCCCNC(=O)C4CCC5C6=C(CCN5C4)C7=CC=CC=C7N6
CHEMBL3423405 drd1_human Human No 5.5 Kd = 3400 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
794 17 7 7 3.1 CCCCC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CC(CC3C(=O)N)N)NC(=O)CCCCCNC(=O)C4CCC5C6=C(CCN5C4)C7=CC=CC=C7N6
CHEMBL3423401 drd1_human Human No 4.4 Kd = 38000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
787 22 8 8 3.3 CCCCC(C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CCCCN)C(=O)N)NC(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL3423401 drd1_human Human No 4.4 Kd = 38000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
787 22 8 8 3.3 CCCCC(C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CCCCN)C(=O)N)NC(=O)CCCCCNC(=O)C2CCC3C4=C(CCN3C2)C5=CC=CC=C5N4
CHEMBL34095 drd1_human Human No 6.4 Kd = 384 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
374 3 2 3 4.3 C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Br
CHEMBL3423408 drd1_human Human No 5.4 Kd = 4000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
773 17 6 8 3.1 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CC(CC2C(=O)N)N)NC(=O)CCCCCNC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL3423408 drd1_human Human No 5.4 Kd = 4000 Funct
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
773 17 6 8 3.1 CCCCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CC(CC2C(=O)N)N)NC(=O)CCCCCNC(=O)C3CCC4C5=C(CCN4C3)C6=CC=CC=C6N5
CHEMBL611801 drd1_human Human Yes 5.3 Kd = 4600 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
207 1 2 3 2.0 CN(C)C1CCC2=CC(=C(C=C2C1)O)O
CHEMBL388509 drd1_human Human No 6.2 Kd = 600 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
629 9 4 6 3.1 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL388509 drd1_human Human No 6.2 Kd = 600 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
629 9 4 6 3.1 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL53 drd1_human Human Yes 6.2 Kd = 680 Funct
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL390299 drd1_human Human No 6.2 Kd = 700 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
736 10 4 8 3.5 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)NC(CC5=CC=C(C=C5)[N+](=O)[O-])C(=O)NC(CC6=CC=C(C=C6)F)C(=O)N7CCCC(C7)C(=O)N
CHEMBL436797 drd1_human Human No 6.2 Kd = 700 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
656 9 4 7 2.8 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL390299 drd1_human Human No 6.2 Kd = 700 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
736 10 4 8 3.5 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)NC(CC5=CC=C(C=C5)[N+](=O)[O-])C(=O)NC(CC6=CC=C(C=C6)F)C(=O)N7CCCC(C7)C(=O)N
CHEMBL436797 drd1_human Human No 6.2 Kd = 700 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
656 9 4 7 2.8 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL388732 drd1_human Human No 5.1 Kd = 7800 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
656 9 4 7 2.8 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL388732 drd1_human Human No 5.1 Kd = 7800 Funct
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
656 9 4 7 2.8 CC(C)C(C(=O)NC(CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)N2CCCC2C(=O)N)NC(=O)C3CN(C4CC5=CNC6=CC=CC(=C56)C4=C3)C
CHEMBL441618 drd1_rat Rat Yes 10.1 Ki = 0.1 Funct
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
290 0 1 1 4.3 CN1CCC2=CC=CC=C2CC3=C(CC1)C4=CC=CC=C4N3
CHEMBL62 drd1_human Human Yes 10.0 Ki = 0.1 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 10.0 Ki = 0.1 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.9 Ki = 0.1 Funct
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.9 Ki = 0.1 Funct
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL596824 drd1_human Human No 9.7 Ki = 0.2 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
413 4 1 3 4.2 CC(=O)N(CC1=CC=C(C=C1)C2CN(CCC3=CC(=C(C=C23)O)Cl)C)C4CCC4
CHEMBL599135 drd1_human Human No 9.7 Ki = 0.2 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
447 4 1 4 6.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C=NOCC5=CC=CC=C5)O)Cl
CHEMBL599528 drd1_human Human No 9.7 Ki = 0.2 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
390 1 1 2 6.1 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=CC=C5)O)Cl
CHEMBL596824 drd1_human Human No 9.7 Ki = 0.2 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
413 4 1 3 4.2 CC(=O)N(CC1=CC=C(C=C1)C2CN(CCC3=CC(=C(C=C23)O)Cl)C)C4CCC4
CHEMBL599135 drd1_human Human No 9.7 Ki = 0.2 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
447 4 1 4 6.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C=NOCC5=CC=CC=C5)O)Cl
CHEMBL599528 drd1_human Human No 9.7 Ki = 0.2 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
390 1 1 2 6.1 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=CC=C5)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.7 Ki = 0.2 Funct
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL13632 drd1_rat Rat No 9.6 Ki = 0.3 Funct
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
367 1 1 2 4.7 CN1CCC2=CC(=C(C=C2C(C1)C3=CC(=CC=C3)Br)O)Cl
CHEMBL62 drd1_human Human Yes 9.5 Ki = 0.3 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL605127 drd1_human Human No 9.5 Ki = 0.3 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
391 1 1 3 5.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=NC=C5)O)Cl
CHEMBL324017 drd1_human Human Yes 9.5 Ki = 0.3 Funct
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
332 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br
CHEMBL300647 drd1_human Human Yes 9.5 Ki = 0.3 Funct
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
336 1 0 1 5.9 CN(C)C1CCC2(C=C1)C3=CC=CC=C3C=CC4=C2C=C(C=C4)Cl
CHEMBL62 drd1_human Human Yes 9.5 Ki = 0.3 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.5 Ki = 0.3 Funct
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.5 Ki = 0.3 Funct
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL605127 drd1_human Human No 9.5 Ki = 0.3 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
391 1 1 3 5.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=NC=C5)O)Cl
CHEMBL201170 drd1_human Human No 9.5 Ki = 0.4 Funct
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.5 Ki = 0.4 Funct
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL62 drd1_human Human Yes 9.4 Ki = 0.4 Funct
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL62 drd1_rat Rat Yes 9.4 Ki = 0.4 Funct
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL304535 drd1_human Human No 9.4 Ki = 0.4 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
302 1 1 2 4.3 CC1=CC=CC(=C1)C2CN(CCC3=CC(=C(C=C23)O)Cl)C
CHEMBL62 drd1_mouse Mouse Yes 9.4 Ki = 0.4 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL598104 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
408 1 1 3 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC(=CC=C5)F)O)Cl
CHEMBL304535 drd1_human Human No 9.4 Ki = 0.4 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
302 1 1 2 4.3 CC1=CC=CC(=C1)C2CN(CCC3=CC(=C(C=C23)O)Cl)C
CHEMBL62 drd1_mouse Mouse Yes 9.4 Ki = 0.4 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.4 Ki = 0.4 Funct
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL201170 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
267 0 1 2 3.8 CN1CCC2=CC=CC=C2CC3=C(CC1)C=C(C=C3)O
CHEMBL598104 drd1_human Human No 9.4 Ki = 0.4 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
408 1 1 3 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC(=CC=C5)F)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.4 Ki = 0.4 Funct
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.4 Ki = 0.4 Funct
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.4 Ki = 0.4 Funct
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.4 Ki = 0.4 Funct
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL380464 drd1_human Human No 9.3 Ki = 0.5 Funct
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
302 0 1 2 4.4 CN1CCC2=C(CC3=CC=CC=C3CC1)C(=C(C=C2)O)Cl
CHEMBL203637 drd1_human Human No 9.3 Ki = 0.5 Funct
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
302 0 1 2 4.4 CN1CCC2=CC=CC=C2CC3=C(CC1)C(=C(C=C3)O)Cl
CHEMBL380464 drd1_human Human No 9.3 Ki = 0.5 Funct
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
302 0 1 2 4.4 CN1CCC2=C(CC3=CC=CC=C3CC1)C(=C(C=C2)O)Cl
CHEMBL203637 drd1_human Human No 9.3 Ki = 0.5 Funct
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
302 0 1 2 4.4 CN1CCC2=CC=CC=C2CC3=C(CC1)C(=C(C=C3)O)Cl
CHEMBL87734 drd1_rat Rat No 9.3 Ki = 0.5 Funct
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
287 2 4 5 1.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC(=CC=C3)O
CHEMBL599282 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
449 5 1 5 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C4CCC4)S(=O)(=O)C)O)Cl
CHEMBL597909 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
407 2 2 5 3.4 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC(=C4)NS(=O)(=O)C)O)Cl
CHEMBL603901 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
409 4 1 5 3.1 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C)S(=O)(=O)C)O)Cl
CHEMBL62 drd1_pig Pig Yes 9.3 Ki = 0.5 Funct
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL599282 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
449 5 1 5 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C4CCC4)S(=O)(=O)C)O)Cl
CHEMBL597909 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
407 2 2 5 3.4 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC(=C4)NS(=O)(=O)C)O)Cl
CHEMBL603901 drd1_human Human No 9.3 Ki = 0.5 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
409 4 1 5 3.1 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C)S(=O)(=O)C)O)Cl
CHEMBL62 drd1_pig Pig Yes 9.3 Ki = 0.5 Funct
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL245570 drd1_human Human No 9.3 Ki = 0.6 Funct
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
306 0 2 2 4.0 CN1CCC2=CC=CC=C2CC3=C(CC1)C4=C(N3)C=CC(=C4)O
CHEMBL245570 drd1_human Human No 9.3 Ki = 0.6 Funct
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
306 0 2 2 4.0 CN1CCC2=CC=CC=C2CC3=C(CC1)C4=C(N3)C=CC(=C4)O
CHEMBL245570 drd1_human Human No 9.3 Ki = 0.6 Funct
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
306 0 2 2 4.0 CN1CCC2=CC=CC=C2CC3=C(CC1)C4=C(N3)C=CC(=C4)O
CHEMBL245570 drd1_human Human No 9.3 Ki = 0.6 Funct
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
306 0 2 2 4.0 CN1CCC2=CC=CC=C2CC3=C(CC1)C4=C(N3)C=CC(=C4)O
CHEMBL3697581 drd1_human Human No 9.2 Ki = 0.6 Funct
BindingDB_Patents: Competition Binding Assay. The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.BindingDB_Patents: Competition Binding Assay. The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
433 3 1 4 3.4 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)I)C3=C(C(=O)NN=C3C)C
CHEMBL3697581 drd1_human Human No 9.2 Ki = 0.6 Funct
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
433 3 1 4 3.4 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)I)C3=C(C(=O)NN=C3C)C
CHEMBL599487 drd1_human Human No 9.2 Ki = 0.6 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
471 5 1 5 4.6 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C)S(=O)(=O)C4=CC=CC=C4)O)Cl
CHEMBL597503 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
429 1 2 2 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC6=C(C=C5)NC=C6)O)Cl
CHEMBL598105 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
415 1 1 3 5.8 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=CC(=C5)C#N)O)Cl
CHEMBL604314 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
330 0 2 3 4.1 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC=C4O)O)Cl
CHEMBL605339 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
435 1 1 4 5.9 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC(=CC=C5)[N+](=O)[O-])O)Cl
CHEMBL599487 drd1_human Human No 9.2 Ki = 0.6 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
471 5 1 5 4.6 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(C)S(=O)(=O)C4=CC=CC=C4)O)Cl
CHEMBL597503 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
429 1 2 2 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC6=C(C=C5)NC=C6)O)Cl
CHEMBL598105 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
415 1 1 3 5.8 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=CC(=C5)C#N)O)Cl
CHEMBL604314 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
330 0 2 3 4.1 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC=C4O)O)Cl
CHEMBL605339 drd1_human Human No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
435 1 1 4 5.9 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC(=CC=C5)[N+](=O)[O-])O)Cl
CHEMBL393466 drd1_rat Rat No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
558 10 0 7 5.5 C1CN2CC3C(CC2CN1CCCC(=O)C4=CC=C(C=C4)F)C5=CC=CC=C5N3CCCC(=O)C6=CC=C(C=C6)F
CHEMBL393466 drd1_rat Rat No 9.2 Ki = 0.6 Funct
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
558 10 0 7 5.5 C1CN2CC3C(CC2CN1CCCC(=O)C4=CC=C(C=C4)F)C5=CC=CC=C5N3CCCC(=O)C6=CC=C(C=C6)F
CHEMBL597702 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
519 6 1 5 7.3 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(CC4=CC=CC=C4)C5=C(C=C(C=C5)F)F)O)Cl
CHEMBL600986 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
421 3 2 5 3.8 CCS(=O)(=O)NC1=CC2=C(C=C1)C3C(CC2)N(CCC4=CC(=C(C=C34)O)Cl)C
CHEMBL599977 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
517 2 3 3 6.3 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC(=C4)NC(=O)NC5=C(C=CC=C5Cl)Cl)O)Cl
CHEMBL603872 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
420 2 1 3 6.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)OC)O)Cl
CHEMBL597310 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
433 2 1 3 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)N(C)C)O)Cl
CHEMBL604176 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
420 2 2 3 5.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)CO)O)Cl
CHEMBL597702 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
519 6 1 5 7.3 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=C(C=C3)CN(CC4=CC=CC=C4)C5=C(C=C(C=C5)F)F)O)Cl
CHEMBL600986 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
421 3 2 5 3.8 CCS(=O)(=O)NC1=CC2=C(C=C1)C3C(CC2)N(CCC4=CC(=C(C=C34)O)Cl)C
CHEMBL599977 drd1_human Human No 9.2 Ki = 0.7 Funct
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
517 2 3 3 6.3 CN1CCC2=CC(=C(C=C2C3C1CCC4=C3C=CC(=C4)NC(=O)NC5=C(C=CC=C5Cl)Cl)O)Cl
CHEMBL13325 drd1_rat Rat No 9.2 Ki = 0.7 Funct
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
367 1 1 2 4.7 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3Br)O)Cl
CHEMBL603872 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
420 2 1 3 6.0 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)OC)O)Cl
CHEMBL597310 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
433 2 1 3 6.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)N(C)C)O)Cl
CHEMBL604176 drd1_human Human No 9.2 Ki = 0.7 Funct
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
420 2 2 3 5.2 CN1CCC2=CC(=C(C=C2C3C1CCC4=C(C=CC=C34)C5=CC=C(C=C5)CO)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.1 Ki = 0.7 Funct
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_rat Rat Yes 9.1 Ki = 0.7 Funct
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL62 drd1_human Human Yes 9.1 Ki = 0.8 Funct
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
288 1 1 2 4.0 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Cl
CHEMBL444321 drd1_human Human No 9.1 Ki = 0.8 Funct
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
302 1 1 2 4.3 CC1=CC=CC=C1C2CN(CCC3=CC(=C(C=C23)O)Cl)C
CHEMBL62 drd1_human Human Yes 9.1 Ki = 0.8