Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10020353 13761 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL1196161 13761 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL556024 13761 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
133538 3549 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
8443 3549 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL574558 3549 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
146025713 171035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025713 171035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171035 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165861 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165861 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165861 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165861 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75202022 170233 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
CHEMBL4453318 170233 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
16219951 171484 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL4472022 171484 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
75202022 170233 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 170233 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
173871 3544 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
936 3544 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL1193571 3544 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
46869265 16066 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 16066 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
10742 3547 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
1225 3547 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL35354 3547 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
92044504 171151 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171151 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
92044504 171151 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171151 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
1241 99703 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL288090 99703 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL552611 99703 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
44320092 161327 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 161327 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
167715 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2820 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
1242 3543 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
935 3543 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL286080 3543 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
10506 2478 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
86290953 2478 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
CHEMBL3421729 2478 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
135 168705 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
3702506 168705 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
CHEMBL441343 168705 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
75201961 169052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 169052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
75201961 169052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 169052 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
146025701 169994 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 169994 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025701 169994 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 169994 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
44320024 106571 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315750 106571 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 174688 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174688 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
44320050 106335 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
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
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 106335 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
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
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 174688 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174688 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
146025715 175612 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 175612 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025715 175612 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 175612 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
6077 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
CHEMBL86931 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
90134269 173624 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 173624 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
75201899 171340 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 171340 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
71722299 101994 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 101994 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 101994 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
44282985 119961 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 119961 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
146025707 170531 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 170531 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320256 204580 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87172 204580 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
13720688 11434 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180542 11434 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL129634 11434 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025696 169125 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 169125 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
44331742 4359 0 None - 1 Rat 6.0 pEC50 = 6 Functional
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
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
CHEMBL101617 4359 0 None - 1 Rat 6.0 pEC50 = 6 Functional
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
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
14708665 167631 1 None - 1 Rat 5.0 pEC50 = 5 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL43345 167631 1 None - 1 Rat 5.0 pEC50 = 5 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
146025696 169125 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 169125 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
146025707 170531 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 170531 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165861 14 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165861 14 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146034919 191592 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204559 191592 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
146025721 171133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 171133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
10684715 160081 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
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
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL41132 160081 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
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
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
71563083 87130 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335737 87130 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
75201901 165861 14 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
CHEMBL4277264 165861 14 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
146025721 171133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 171133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
44276535 97924 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL275379 97924 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
44417647 81735 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 81735 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 81735 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
24878061 140867 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 140867 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
146025709 173999 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 173999 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145982261 166168 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4283176 166168 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
146192959 169937 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449550 169937 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
44282985 119961 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 119961 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
130442557 166509 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4289538 166509 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
146025709 173999 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 173999 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
71722297 101986 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 101986 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 101986 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
85090332 180127 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 180127 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
90134199 171666 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 171666 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
90134199 171666 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 171666 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
44320303 163404 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420788 163404 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442471 175500 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175500 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
681 1432 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 1432 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 1432 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 1432 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 1432 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
44554468 105774 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099225 105774 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139011 105774 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025716 173383 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 173383 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276651 99266 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL284959 99266 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
85090319 180018 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 180018 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
130442534 166333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286177 166333 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
2030130 20764 13 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 20764 13 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025716 173383 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 173383 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145988779 166715 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
CHEMBL4293356 166715 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
44320328 204496 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
CHEMBL86669 204496 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
10689581 99687 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
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
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL287931 99687 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
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
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
3106 48241 14 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
CHEMBL15564 48241 14 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
168278276 190512 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187937 190512 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146192950 175447 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
CHEMBL4590150 175447 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
168280742 190480 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 190480 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
130442471 175500 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175500 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
146192960 170943 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4464150 170943 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320116 163545 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 163545 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
117720272 118296 1 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
CHEMBL3421730 118296 1 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
1242 3543 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
935 3543 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
CHEMBL286080 3543 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
146025697 174769 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 174769 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
168276676 189858 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5178743 189858 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146025697 174769 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 174769 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
130442561 166329 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286110 166329 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
161665 172006 33 None -28 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 172006 33 None -28 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
85090324 180100 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 180100 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
6603820 95317 13 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL25856 95317 13 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
146025712 174900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 174900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
10666053 99908 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
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
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289927 99908 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
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
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
146025703 170691 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 170691 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
75201901 165861 14 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165861 14 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146025703 170691 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 170691 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
15696481 79241 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 79241 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
146025712 174900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 174900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
132435 130174 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL130795 130174 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL368456 130174 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025704 171772 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 171772 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44554818 103776 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099234 103776 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44554472 105789 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099226 105789 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139040 105789 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85090328 180443 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 180443 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090323 181330 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 181330 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
146025813 175004 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175004 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025813 175004 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175004 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90134304 165950 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4278861 165950 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
146025821 169093 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169093 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025821 169093 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169093 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 172641 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 172641 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 172641 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 172641 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
85090329 182090 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 182090 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
137364078 191617 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204914 191617 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
3246443 37438 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37438 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
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
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
146025704 171772 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 171772 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320053 204049 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 204049 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
11938 2369 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192952 2369 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4468760 2369 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44287454 13102 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1191276 13102 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL542351 13102 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
146025718 174611 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 174611 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
117720272 118296 1 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 118296 1 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
146025718 174611 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 174611 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
85090333 180709 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 180709 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
76284419 182656 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 182656 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
85090325 179159 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 179159 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
75201901 165861 14 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
CHEMBL4277264 165861 14 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
10854877 141471 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL38757 141471 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10733562 146469 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL39266 146469 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
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
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
1242 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
935 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
CHEMBL286080 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
136326241 178838 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 178838 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
146192966 174734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
CHEMBL4573538 174734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
44319988 204349 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85552 204349 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10758745 99954 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 99954 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 99954 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44276414 97166 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL27101 97166 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
155548298 173169 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4536851 173169 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320001 204287 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 204287 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
935 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
CHEMBL286080 3543 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
146025729 173577 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 173577 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44276652 99021 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL283247 99021 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
146025729 173577 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 173577 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
85090322 178869 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 178869 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090321 182221 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 182221 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168294420 191902 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5209228 191902 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
6603820 95317 13 None 1 7 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 95317 13 None 1 7 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
44554820 105792 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099222 105792 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139044 105792 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025724 171688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 171688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025819 175069 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 175069 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025819 175069 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 175069 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025724 171688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 171688 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
85090334 180033 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 180033 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090331 180861 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 180861 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
12668019 10128 6 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL1160787 10128 6 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
44320061 105539 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313304 105539 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
14809027 106533 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 106533 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
146025727 171109 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171109 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025727 171109 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171109 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171332 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171332 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171332 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171332 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10506 2478 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 2478 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 2478 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
130442473 166772 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166772 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 166772 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166772 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
1153 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
12668023 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026874 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026875 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
3341 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
6603851 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
933 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
939 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
985 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1160786 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1161520 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL588 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
DB00800 1591 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
681 1432 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
940 1432 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
947 1432 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
CHEMBL59 1432 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
DB00988 1432 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
75201899 171340 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
CHEMBL4469983 171340 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
201536 110967 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 110967 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
201536 110967 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 110967 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
133741 197378 8 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
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
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
CHEMBL587 197378 8 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
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
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
90134211 173447 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 173447 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
71722293 101989 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 101989 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 101989 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
44554984 103773 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099231 103773 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155541775 172465 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 172465 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
137364059 189716 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5176312 189716 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
168289194 190888 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193714 190888 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
10662054 83977 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114444 83977 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219803 83977 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
90134211 173447 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 173447 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
155519631 169826 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 169826 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
145979741 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4282096 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
6917970 3622 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
8370 3622 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
CHEMBL487387 3622 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
44276412 97203 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL27117 97203 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44320116 163545 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
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
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 163545 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
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
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44554649 103777 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099235 103777 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44276557 98845 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL282136 98845 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
21936384 190906 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193924 190906 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
681 1432 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
940 1432 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
947 1432 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
CHEMBL59 1432 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
DB00988 1432 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
15696482 79134 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2114209 79134 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
85090326 182181 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 182181 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
44320218 204688 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
CHEMBL87897 204688 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
146025811 171185 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171185 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025811 171185 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171185 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10640108 83976 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114441 83976 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219802 83976 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
9841398 99045 3 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL28338 99045 3 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
44320267 204480 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 204480 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10588327 13654 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1195441 13654 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL554571 13654 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
145990190 166289 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4285528 166289 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
85090337 182689 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 182689 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
21786101 155179 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
CHEMBL405519 155179 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
1241 99703 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL288090 99703 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL552611 99703 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
228 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
155541775 172465 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 172465 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
145979741 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
CHEMBL4282096 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
145979741 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
CHEMBL4282096 166121 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
4901726 180207 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 180207 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025714 169719 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 169719 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025714 169719 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 169719 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 166772 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4294397 166772 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
146025730 171392 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 171392 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025730 171392 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 171392 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
9796958 146033 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 146033 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 146033 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 146033 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44320304 106539 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
CHEMBL315516 106539 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
85090318 178855 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 178855 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
10758744 100028 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL291100 100028 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
10710466 155862 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL40667 155862 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
2407 3308 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
59227 3308 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
941 3308 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL1303 3308 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
DB05271 3308 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
146192958 169936 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449549 169936 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192964 174128 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4559891 174128 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
10519435 170893 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL446350 170893 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
15981509 141414 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 141414 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
10856744 59695 10 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
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.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
CHEMBL17357 59695 10 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
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.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
85090330 180481 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 180481 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
10506 2478 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 2478 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 2478 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
44320050 106335 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 106335 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44320357 204663 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 204663 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86293768 118297 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421836 118297 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
228 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6604773 16067 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
CHEMBL1224528 16067 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
228 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6852376 91153 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL1467585 91153 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL24077 91153 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL503958 91153 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
6603820 95317 13 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL25856 95317 13 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
145867041 173947 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4555682 173947 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
44320327 162860 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 162860 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 3543 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 3543 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 3543 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
137364067 190471 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187471 190471 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
10709445 100880 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 100880 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 100880 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
3033200 173945 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173945 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
3033200 173945 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173945 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
117720272 118296 1 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 118296 1 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
71722291 101974 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397385 101974 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040059 101974 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
146025708 172942 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 172942 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
25142456 81980 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81980 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
146025708 172942 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 172942 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276404 98608 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL28054 98608 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
10802235 13133 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1191487 13133 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL542593 13133 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
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
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
10732044 83978 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114440 83978 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219804 83978 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
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
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
75201901 165861 14 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165861 14 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
44554474 105791 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099227 105791 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139043 105791 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155519631 169826 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 169826 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
146025818 169184 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4438800 169184 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575