Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL3234541 drd2_human Human No 6.0 AC50 = 1020 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234541 drd2_human Human No 6.0 AC50 = 1020 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234511 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
420 4 1 5 2.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234238 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=CC=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234537 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234524 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
412 4 1 5 2.0 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234511 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
420 4 1 5 2.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234238 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=CC=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234537 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234524 drd2_human Human No 7.0 AC50 = 112 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
412 4 1 5 2.0 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234520 drd2_human Human No 5.0 AC50 = 11200 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=N3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234520 drd2_human Human No 5.0 AC50 = 11200 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=N3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234527 drd2_human Human No 5.9 AC50 = 1150 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234527 drd2_human Human No 5.9 AC50 = 1150 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234538 drd2_human Human No 5.9 AC50 = 1290 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
497 4 1 4 4.0 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234538 drd2_human Human No 5.9 AC50 = 1290 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
497 4 1 4 4.0 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234508 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
420 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234517 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234503 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234527 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234502 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
472 4 1 7 3.8 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C(F)(F)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234508 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
420 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234517 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234503 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234527 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234502 drd2_human Human No 6.9 AC50 = 141 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
472 4 1 7 3.8 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C(F)(F)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234513 drd2_human Human No 5.8 AC50 = 1580 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
376 2 1 4 2.6 CN1C2=C(C=CC(=C2)C(=O)NC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234513 drd2_human Human No 5.8 AC50 = 1580 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
376 2 1 4 2.6 CN1C2=C(C=CC(=C2)C(=O)NC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL1529544 drd2_human Human Yes 6.8 AC50 = 177 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 4 1 4 3.3 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL1529544 drd2_human Human Yes 6.8 AC50 = 177 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 4 1 4 3.3 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234505 drd2_human Human No 5.8 AC50 = 1770 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
495 7 1 7 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=C(C(=C3)OC)OC)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234505 drd2_human Human No 5.8 AC50 = 1770 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
495 7 1 7 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=C(C(=C3)OC)OC)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234535 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)NC(=O)CC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234538 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
497 4 1 4 4.0 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234500 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
451 5 1 5 3.4 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)SC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234515 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
390 3 1 4 2.6 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234535 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)NC(=O)CC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234538 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
497 4 1 4 4.0 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234500 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
451 5 1 5 3.4 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)SC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234515 drd2_human Human No 6.7 AC50 = 223 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
390 3 1 4 2.6 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234537 drd2_human Human No 6.6 AC50 = 257 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234537 drd2_human Human No 6.6 AC50 = 257 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
429 4 1 5 2.7 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C#N)S(=O)C4=CC=CC=C4C1=O
CHEMBL1503220 drd2_human Human Yes 6.6 AC50 = 280 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234540 drd2_human Human No 6.6 AC50 = 280 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL1503220 drd2_human Human Yes 6.6 AC50 = 280 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234540 drd2_human Human No 6.6 AC50 = 280 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234521 drd2_human Human No 6.6 AC50 = 281 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234518 drd2_human Human No 6.6 AC50 = 281 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=CC=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234521 drd2_human Human No 6.6 AC50 = 281 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234518 drd2_human Human No 6.6 AC50 = 281 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC(=CC=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL1503220 drd2_human Human Yes 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234539 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
469 4 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC4=CC=CC=C4C=C3)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234540 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234542 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL1503220 drd2_human Human Yes 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234539 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
469 4 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC4=CC=CC=C4C=C3)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234540 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
425 3 1 4 3.2 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234542 drd2_human Human No 5.5 AC50 = 2890 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234509 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
449 6 1 5 3.4 CCN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234516 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
408 3 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234539 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 4 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC4=CC=CC=C4C=C3)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234514 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
406 3 1 5 2.6 CN1C2=C(C=CC(=C2)C(=O)NC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234506 drd2_human Human Yes 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
448 4 1 6 2.8 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC4=C(C=C3)OCO4)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234504 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
483 5 1 6 2.2 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)S(=O)(=O)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234501 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
461 5 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C(C)(C)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234509 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
449 6 1 5 3.4 CCN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234516 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
408 3 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234539 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 4 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC4=CC=CC=C4C=C3)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234514 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
406 3 1 5 2.6 CN1C2=C(C=CC(=C2)C(=O)NC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234506 drd2_human Human Yes 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
448 4 1 6 2.8 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC4=C(C=C3)OCO4)S(=O)C5=CC=CC=C5C1=O
CHEMBL3234504 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
483 5 1 6 2.2 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)S(=O)(=O)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234501 drd2_human Human No 6.5 AC50 = 353 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
461 5 1 4 4.6 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)C(C)(C)C)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234543 drd2_human Human No 6.4 AC50 = 363 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234543 drd2_human Human No 6.4 AC50 = 363 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234542 drd2_human Human No 6.4 AC50 = 445 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234239 drd2_human Human No 6.4 AC50 = 445 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
404 4 1 4 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234542 drd2_human Human No 6.4 AC50 = 445 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
391 3 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCC3=CN=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234239 drd2_human Human No 6.4 AC50 = 445 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
404 4 1 4 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL1726600 drd2_human Human Yes 5.4 AC50 = 4460 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL1726600 drd2_human Human Yes 5.4 AC50 = 4460 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL1714249 drd2_human Human Yes 6.3 AC50 = 509 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
439 4 1 4 3.6 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL1714249 drd2_human Human Yes 6.3 AC50 = 509 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
439 4 1 4 3.6 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Cl)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234536 drd2_human Human No 7.3 AC50 = 56 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234536 drd2_human Human No 7.3 AC50 = 56 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234499 drd2_human Human Yes 6.3 AC50 = 560 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 4 1 4 3.3 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234525 drd2_human Human No 6.3 AC50 = 560 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
385 5 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCCCN(C)C)S(=O)C3=CC=CC=C3C1=O
CHEMBL3234499 drd2_human Human Yes 6.3 AC50 = 560 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 4 1 4 3.3 CCN1C2=C(C=CC(=C2)C(=O)NC(C)C3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234525 drd2_human Human No 6.3 AC50 = 560 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
385 5 1 5 1.5 CN1C2=C(C=CC(=C2)C(=O)NCCCN(C)C)S(=O)C3=CC=CC=C3C1=O
CHEMBL3234532 drd2_human Human No 4.3 AC50 = 56000 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
433 5 0 4 3.5 CCN1C2=C(C=CC(=C2)C(=O)N(CC)CC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234532 drd2_human Human No 4.3 AC50 = 56000 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
433 5 0 4 3.5 CCN1C2=C(C=CC(=C2)C(=O)N(CC)CC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234536 drd2_human Human No 6.2 AC50 = 576 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234536 drd2_human Human No 6.2 AC50 = 576 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234543 drd2_human Human No 7.2 AC50 = 70 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234544 drd2_human Human Yes 7.2 AC50 = 70 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234543 drd2_human Human No 7.2 AC50 = 70 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234544 drd2_human Human Yes 7.2 AC50 = 70 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234512 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
449 6 1 5 3.4 CCCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234526 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 5 1 4 4.2 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)SC4=CC=CC=C4C1=O
CHEMBL3234534 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)NC(=O)CC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234512 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
449 6 1 5 3.4 CCCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234526 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
419 5 1 4 4.2 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)OC)SC4=CC=CC=C4C1=O
CHEMBL3234534 drd2_human Human No 6.2 AC50 = 705 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
435 5 1 5 2.9 CCN1C2=C(C=CC(=C2)NC(=O)CC3=CC=C(C=C3)OC)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234519 drd2_human Human No 7.2 AC50 = 71 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234519 drd2_human Human No 7.2 AC50 = 71 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234544 drd2_human Human Yes 6.1 AC50 = 725 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234544 drd2_human Human Yes 6.1 AC50 = 725 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234507 drd2_human Human No 6.1 AC50 = 887 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
390 3 1 4 3.0 CCN1C2=C(C=CC(=C2)C(=O)NC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234510 drd2_human Human No 6.1 AC50 = 887 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
406 4 2 5 2.4 COC1=CC=C(C=C1)CNC(=O)C2=CC3=C(C=C2)S(=O)C4=CC=CC=C4C(=O)N3
CHEMBL3234507 drd2_human Human No 6.1 AC50 = 887 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
390 3 1 4 3.0 CCN1C2=C(C=CC(=C2)C(=O)NC3=CC=CC=C3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234510 drd2_human Human No 6.1 AC50 = 887 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
406 4 2 5 2.4 COC1=CC=C(C=C1)CNC(=O)C2=CC3=C(C=C2)S(=O)C4=CC=CC=C4C(=O)N3
CHEMBL1703877 drd2_human Human Yes 5.1 AC50 = 8870 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
497 6 1 5 4.0 COC1=CC=C(C=C1)CNC(=O)C2=CC3=C(C=C2)S(=O)C4=CC=CC=C4C(=O)N3CC5=CC=CC=C5
CHEMBL1703877 drd2_human Human Yes 5.1 AC50 = 8870 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
497 6 1 5 4.0 COC1=CC=C(C=C1)CNC(=O)C2=CC3=C(C=C2)S(=O)C4=CC=CC=C4C(=O)N3CC5=CC=CC=C5
CHEMBL1894173 drd2_human Human Yes 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234522 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234523 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234541 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL1894173 drd2_human Human Yes 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
422 4 1 5 3.0 CCN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)F)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234522 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234523 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
397 4 1 5 1.6 CN1C2=C(C=CC(=C2)C(=O)NCCN3CCCC3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234541 drd2_human Human No 7.1 AC50 = 89 Funct
Antagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysisAntagonist activity at D2 receptor (unknown origin) expressed in Flp-In TREx 293 cells coexpressing chimeric Gqi5 protein assessed as calcium accumulation by Fluo-8AM dye based fluorescence analysis
469 3 1 4 3.3 CN1C2=C(C=CC(=C2)C(=O)NCC3=CC=C(C=C3)Br)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234522 drd2_human Human No 6.0 AC50 = 913 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL3234522 drd2_human Human No 6.0 AC50 = 913 Funct
Antagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
411 4 1 5 2.7 CN1C2=C(C=CC(=C2)C(=O)NCCC3=CC=CS3)S(=O)C4=CC=CC=C4C1=O
CHEMBL98305 drd2_rat Rat No 10.9 EC50 = 0.0 Funct
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
265 2 1 4 2.5 CCCN1CCOC2C1CSC3=C2C=C(C=C3)O
CHEMBL379602 drd2_human Human Yes 9.7 EC50 = 0.2 Funct
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
348 5 0 4 3.3 COC1=CC=CC=C1N2CCN(CC2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL379602 drd2_human Human Yes 9.7 EC50 = 0.2 Funct
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
348 5 0 4 3.3 COC1=CC=CC=C1N2CCN(CC2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL379602 drd2_human Human Yes 9.6 EC50 = 0.3 Funct
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
348 5 0 4 3.3 COC1=CC=CC=C1N2CCN(CC2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL379602 drd2_human Human Yes 9.6 EC50 = 0.3 Funct
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
348 5 0 4 3.3 COC1=CC=CC=C1N2CCN(CC2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL3298895 drd2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
521 8 2 6 6.4 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)N)C
CHEMBL3798179 drd2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3298895 drd2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated for 30 mins by AlphaScreen assay
521 8 2 6 6.4 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)N)C
CHEMBL160630 drd2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
397 7 1 5 3.5 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4F
CHEMBL431367 drd2_human Human Yes 9.4 EC50 = 0.4 Funct
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
346 6 2 2 4.6 C1CN(CC=C1C2=CC=CC=C2)CCCCC3=CNC4=C3C=C(C=C4)O
CHEMBL3299094 drd2_human Human No 9.4 EC50 = 0.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
349 8 1 5 2.9 CC(C)(C)OC(=O)NCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3299094 drd2_human Human No 9.4 EC50 = 0.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
349 8 1 5 2.9 CC(C)(C)OC(=O)NCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3299094 drd2_human Human No 9.4 EC50 = 0.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
349 8 1 5 2.9 CC(C)(C)OC(=O)NCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL53 drd2_rat Rat Yes 9.4 EC50 = 0.4 Funct
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL160357 drd2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
380 7 1 4 3.4 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4
CHEMBL53 drd2_rat Rat Yes 9.4 EC50 = 0.4 Funct
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_rat Rat Yes 9.4 EC50 = 0.4 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL2206265 drd2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
549 17 2 4 9.8 CCCN(CCCCCCCCCCN(CCC)C1CCC2=C(C1)C=CC=C2O)C3CCC4=C(C3)C=CC=C4O
CHEMBL160296 drd2_human Human No 9.3 EC50 = 0.5 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
410 8 1 5 3.4 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3099235 drd2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
328 4 1 5 2.3 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=NC=N4
CHEMBL108531 drd2_human Human Yes 9.3 EC50 = 0.5 Funct
Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals)
302 4 1 2 4.5 C1CN(CC=C1C2=CC=CC=C2)CCC#CC3=CC=C(C=C3)N
CHEMBL109063 drd2_human Human No 9.3 EC50 = 0.5 Funct
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
303 4 1 3 3.1 C1CN(CC=C1C2=CC=CC=C2)CCC#CC3=CN=C(C=C3)N
CHEMBL1765633 drd2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL1765633 drd2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrsAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as induction of [3H]thymidine incorporation after 2 hrs
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL3299095 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
364 9 1 5 3.2 CC(C)(C)OC(=O)NCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL160296 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
410 8 1 5 3.4 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3299095 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
364 9 1 5 3.2 CC(C)(C)OC(=O)NCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3299095 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
364 9 1 5 3.2 CC(C)(C)OC(=O)NCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL1081489 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
287 4 0 2 2.3 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC=CC=C3
CHEMBL1085672 drd2_human Human No 9.2 EC50 = 0.6 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
294 3 1 2 2.2 C1CCNC(C1)CN2CCN(C2=O)C3=CC(=CC=C3)Cl
CHEMBL405519 drd2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
261 2 2 3 3.2 CCCN1CCCC2C1CC3=C(C2)C(=C(C=C3)O)O
CHEMBL405519 drd2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
261 2 2 3 3.2 CCCN1CCCC2C1CC3=C(C2)C(=C(C=C3)O)O
CHEMBL1303 drd2_human Human Yes 9.2 EC50 = 0.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
316 6 1 3 4.9 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
CHEMBL1081490 drd2_human Human No 9.1 EC50 = 0.8 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
305 4 0 3 2.4 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC(=CC=C3)F
CHEMBL160921 drd2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
405 7 1 5 3.1 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4C#N
CHEMBL160630 drd2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
397 7 1 5 3.5 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4F
CHEMBL443034 drd2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
424 9 1 5 3.7 CCOC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL160357 drd2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
380 7 1 4 3.4 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4
CHEMBL3797209 drd2_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL3797209 drd2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL434665 drd2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL1077344 drd2_human Human No 9.0 EC50 = 1 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
322 4 0 2 2.9 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC(=CC=C3)Cl
CHEMBL2165120 drd2_human Human No 9.0 EC50 = 1 Funct
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
460 7 1 4 5.3 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)C=CC(=O)N4
CHEMBL3099231 drd2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
327 4 1 4 2.6 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC=N4
CHEMBL434665 drd2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL110489 drd2_human Human No 9.0 EC50 = 1 Funct
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
288 4 0 2 4.1 C1CN(CC=C1C2=CC=CC=C2)CCC#CC3=CC=NC=C3
CHEMBL1077344 drd2_human Human No 9.0 EC50 = 1 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
322 4 0 2 2.9 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC(=CC=C3)Cl
CHEMBL3798179 drd2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL109101 drd2_human Human No 8.9 EC50 = 1.3 Funct
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
303 4 1 3 2.8 C1CN(CC=C1C2=CC=CC=C2)CCC#CC3=NC=C(C=C3)N
CHEMBL3577346 drd2_human Human No 8.9 EC50 = 1.4 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL3577346 drd2_human Human No 8.9 EC50 = 1.4 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL2323579 drd2_human Human No 8.9 EC50 = 1.4 Funct
Partial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysisPartial agonist activity at human D2 receptor transfected in HTLA cells measured after overnight incubation by luminescence counter analysis
440 6 1 4 2.7 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CN(C4=CC=CC2=C34)C)N(C1)C
CHEMBL3299096 drd2_human Human No 8.9 EC50 = 1.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
378 10 1 5 3.6 CC(C)(C)OC(=O)NCCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3299096 drd2_human Human No 8.8 EC50 = 1.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
378 10 1 5 3.6 CC(C)(C)OC(=O)NCCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3299096 drd2_human Human No 8.8 EC50 = 1.4 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
378 10 1 5 3.6 CC(C)(C)OC(=O)NCCCCCN1CCN(CC1)C2=CC=CC=C2OC
CHEMBL3099230 drd2_human Human No 8.8 EC50 = 1.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
327 4 1 4 2.6 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC=N4
CHEMBL399164 drd2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
424 8 1 5 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2OC)C3CCC4=C(C3)C=CC=C4O
CHEMBL399164 drd2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
424 8 1 5 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2OC)C3CCC4=C(C3)C=CC=C4O
CHEMBL2165119 drd2_human Human Yes 8.8 EC50 = 1.6 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
463 7 1 5 4.6 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=NC4=C(CCC(=O)N4)C=C3
CHEMBL599635 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
461 7 2 6 4.8 CCCN(CCN1CCN(CC1)C2=C3C=CC=C(C3=NC=C2)O)C4CCC5=C(C4)C=C(C=C5)O
CHEMBL599635 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
461 7 2 6 4.8 CCCN(CCN1CCN(CC1)C2=C3C=CC=C(C3=NC=C2)O)C4CCC5=C(C4)C=C(C=C5)O
CHEMBL338606 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
412 9 1 5 4.0 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C=CC3=CC=C(C=C3)F
CHEMBL378455 drd2_human Human No 8.8 EC50 = 1.7 Funct
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL2206264 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
535 16 2 4 9.3 CCCN(CCCCCCCCCN(CCC)C1CCC2=C(C1)C=CC=C2O)C3CCC4=C(C3)C=CC=C4O
CHEMBL3099234 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
328 4 1 5 2.3 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=NC=N4
CHEMBL338606 drd2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporationAgonist activity at human dopamine receptor D2long expressed in CHO10001 cells assessed as stimulation of incorporation [3H]-thymidine incorporation
412 9 1 5 4.0 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C=CC3=CC=C(C=C3)F
CHEMBL53 drd2_human Human Yes 8.8 EC50 = 1.7 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL108463 drd2_human Human No 8.8 EC50 = 1.7 Funct
In vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptorsIn vivo Dopamine receptor D2 mitogenesis measured as [3H]thymidine incorporation in CHO p-5 cells expressing human D2 receptors
288 4 0 2 3.4 C1CN(CC=C1C2=CC=CC=C2)CCC#CC3=CN=CC=C3
CHEMBL378455 drd2_human Human No 8.8 EC50 = 1.7 Funct
Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL53 drd2_human Human Yes 8.7 EC50 = 1.8 Funct
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_human Human Yes 8.8 EC50 = 1.8 Funct
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPRAgonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_rat Rat Yes 8.8 EC50 = 1.8 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL82663 drd2_human Human Yes 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL82663 drd2_human Human Yes 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assayAgonist activity at human recombinant dopamine D2S receptor expressed in HEK cells by GTPgammaS binding assay
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL1083813 drd2_human Human No 8.0 EC50 = 10 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
340 4 0 3 3.0 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC(=C(C=C3)F)Cl
CHEMBL1081311 drd2_human Human No 8.0 EC50 = 10 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
301 4 0 2 2.7 CC1=CC(=CC=C1)N2CCN(C2=O)CCN3CCCCCC3
CHEMBL1081491 drd2_human Human No 8.0 EC50 = 10 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
305 4 0 3 2.4 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC=C(C=C3)F
CHEMBL2165123 drd2_human Human No 8.0 EC50 = 10 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
424 9 1 5 3.7 CCOC1=CC=CC(=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3134061 drd2_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
324 4 2 4 2.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCN)O
CHEMBL273273 drd2_human Human Yes 8.0 EC50 = 10.4 Funct
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C=CC=C2O
CHEMBL273273 drd2_human Human Yes 8.0 EC50 = 10.4 Funct
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C=CC=C2O
CHEMBL335403 drd2_human Human No 8.0 EC50 = 10.4 Funct
In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptorIn vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor
419 4 1 4 4.4 C1CC(CC2C1CC(CC2)N3CCN(CC3)C4=CC=CC=N4)NC(=O)C5=CC=CC=C5
CHEMBL419792 drd2_rat Rat Yes 8.0 EC50 = 10.8 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL2165138 drd2_human Human Yes 7.0 EC50 = 100 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
421 6 0 4 6.2 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCOC3=CC4=C(C=C3)SC=N4
CHEMBL2165134 drd2_human Human No 7.0 EC50 = 100 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
419 7 1 4 5.1 C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=NN3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165129 drd2_human Human No 6.0 EC50 = 1000 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
444 4 1 4 4.0 C1CC(=O)NC2=C1C=CC(=C2)OCC#CCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3597637 drd2_human Human No 5.0 EC50 = 10000 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
453 8 1 5 4.4 COC1=C(C=CC=C1Cl)N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4N=C3
CHEMBL3597637 drd2_human Human No 5.0 EC50 = 10000 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
453 8 1 5 4.4 COC1=C(C=CC=C1Cl)N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4N=C3
CHEMBL3799626 drd2_human Human No 7.0 EC50 = 102 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
467 7 2 3 4.2 CN(CCCCNC(=O)C1=CC2=C(C=C1)C3=CC=CC=C3C2)C4CC5=C6C(=CC=C5)NC(=O)N6C4
CHEMBL3799626 drd2_human Human No 7.0 EC50 = 102 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
467 7 2 3 4.2 CN(CCCCNC(=O)C1=CC2=C(C=C1)C3=CC=CC=C3C2)C4CC5=C6C(=CC=C5)NC(=O)N6C4
CHEMBL86931 drd2_rat Rat Yes 5.0 EC50 = 10200 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL86931 drd2_rat Rat Yes 5.0 EC50 = 10200 Funct
Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobeFormation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL2165139 drd2_human Human No 7.0 EC50 = 107 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
422 6 0 5 5.6 C1CN(CCN1CCCOC2=CC3=C(C=C2)SC=N3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1253770 drd2_human Human No 7.0 EC50 = 108 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
470 8 1 4 6.5 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)C=C(C=C5)O
CHEMBL1253770 drd2_human Human No 7.0 EC50 = 108 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
470 8 1 4 6.5 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)C=C(C=C5)O
CHEMBL2115213 drd2_rat Rat No 5.0 EC50 = 10800 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
223 2 3 4 1.0 CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3799626 drd2_human Human No 7.0 EC50 = 109 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
467 7 2 3 4.2 CN(CCCCNC(=O)C1=CC2=C(C=C1)C3=CC=CC=C3C2)C4CC5=C6C(=CC=C5)NC(=O)N6C4
CHEMBL3799626 drd2_human Human No 7.0 EC50 = 109 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
467 7 2 3 4.2 CN(CCCCNC(=O)C1=CC2=C(C=C1)C3=CC=CC=C3C2)C4CC5=C6C(=CC=C5)NC(=O)N6C4
CHEMBL3287405 drd2_human Human No 7.0 EC50 = 109.7 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
444 7 0 5 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3613878 drd2_human Human No 6.0 EC50 = 1096.5 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
442 5 0 5 3.7 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613878 drd2_human Human No 6.0 EC50 = 1096.5 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
442 5 0 5 3.7 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL316983 drd2_rat Rat No 8.0 EC50 = 11 Funct
Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
248 6 0 2 2.7 CCCN(CCC)C1CCN2C(=CC=C2C=O)C1
CHEMBL316983 drd2_rat Rat No 8.0 EC50 = 11 Funct
Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
248 6 0 2 2.7 CCCN(CCC)C1CCN2C(=CC=C2C=O)C1
CHEMBL3800636 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
422 12 3 5 5.3 COC1=C(C=CC(=C1)CCNCCC2=CC(=C(C=C2)O)O)OCCCC3=CC=CC=C3
CHEMBL2028019 drd2_human Human Yes 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3085826 drd2_human Human Yes 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3287405 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
444 7 0 5 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1765633 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assayAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assay
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL3577342 drd2_human Human No 7.0 EC50 = 110 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3800636 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
422 12 3 5 5.3 COC1=C(C=CC(=C1)CCNCCC2=CC(=C(C=C2)O)O)OCCCC3=CC=CC=C3
CHEMBL2028019 drd2_human Human Yes 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3085826 drd2_human Human Yes 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3287405 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
444 7 0 5 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C#N)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1765633 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assayAgonist activity at human dopamine D2long receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP accumulation by bioluminescence assay
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL3134068 drd2_human Human No 7.0 EC50 = 110 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
843 21 4 8 9.2 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCCCCCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL3577342 drd2_human Human No 7.0 EC50 = 110 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3800341 drd2_human Human No 6.0 EC50 = 1100 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
477 12 3 6 4.6 COC1=C(C=CC(=C1)CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)OCCCC4=CC=CC=C4
CHEMBL3800341 drd2_human Human No 6.0 EC50 = 1100 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
477 12 3 6 4.6 COC1=C(C=CC(=C1)CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)OCCCC4=CC=CC=C4
CHEMBL434665 drd2_human Human Yes 7.0 EC50 = 111.2 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL2028019 drd2_human Human Yes 7.0 EC50 = 112.2 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3085826 drd2_human Human Yes 7.0 EC50 = 112.2 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3394254 drd2_human Human No 7.0 EC50 = 112.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
573 23 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3394254 drd2_human Human No 7.0 EC50 = 112.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
573 23 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3613879 drd2_human Human No 6.0 EC50 = 1122.0 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
456 6 0 5 4.0 C1CN(CCN1CCCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613879 drd2_human Human No 6.0 EC50 = 1122.0 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
456 6 0 5 4.0 C1CN(CCN1CCCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL2152747 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
467 7 2 6 3.8 CCCN(CCN1CCN(CC1)C(=O)C2=CC3=CC=CC=C3N2)C4CCC5=C(C4)SC(=N5)N
CHEMBL241973 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
445 9 1 5 4.1 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC=C(C=C3)C4=CC=CC=N4
CHEMBL3394254 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
573 23 3 5 6.4 CCCN(CCCNC(=O)CCCCCCCCCCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL2115032 drd2_rat Rat Yes 6.9 EC50 = 114 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
297 1 2 4 2.3 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O
CHEMBL2152747 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
467 7 2 6 3.8 CCCN(CCN1CCN(CC1)C(=O)C2=CC3=CC=CC=C3N2)C4CCC5=C(C4)SC(=N5)N
CHEMBL241973 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
445 9 1 5 4.1 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC=C(C=C3)C4=CC=CC=N4
CHEMBL2152746 drd2_human Human No 6.9 EC50 = 114 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
467 7 2 6 3.8 CCCN(CCN1CCN(CC1)C(=O)C2=CC3=CC=CC=C3N2)C4CCC5=C(C4)SC(=N5)N
CHEMBL2115032 drd2_rat Rat Yes 6.9 EC50 = 114 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
297 1 2 4 2.3 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O
CHEMBL571992 drd2_human Human No 6.9 EC50 = 116 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
451 7 1 7 4.5 CCCN(CCN1CCN(CC1)C2=NC=CC3=CC=CC=C32)C4CCC5=C(C4)SC(=N5)N
CHEMBL571992 drd2_human Human No 6.9 EC50 = 116 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
451 7 1 7 4.5 CCCN(CCN1CCN(CC1)C2=NC=CC3=CC=CC=C32)C4CCC5=C(C4)SC(=N5)N
CHEMBL571992 drd2_human Human No 6.9 EC50 = 116 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
451 7 1 7 4.5 CCCN(CCN1CCN(CC1)C2=NC=CC3=CC=CC=C32)C4CCC5=C(C4)SC(=N5)N
CHEMBL571992 drd2_human Human No 6.9 EC50 = 116 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
451 7 1 7 4.5 CCCN(CCN1CCN(CC1)C2=NC=CC3=CC=CC=C32)C4CCC5=C(C4)SC(=N5)N
CHEMBL571992 drd2_human Human No 6.9 EC50 = 116 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
451 7 1 7 4.5 CCCN(CCN1CCN(CC1)C2=NC=CC3=CC=CC=C32)C4CCC5=C(C4)SC(=N5)N
CHEMBL156639 drd2_human Human Yes 7.9 EC50 = 12.2 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
394 7 1 4 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2)C3CCC4=C(C3)C=C(C=C4)O
CHEMBL156639 drd2_human Human Yes 7.9 EC50 = 12.2 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
394 7 1 4 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2)C3CCC4=C(C3)C=C(C=C4)O
CHEMBL53 drd2_human Human Yes 7.9 EC50 = 12.7 Funct
Agonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL434665 drd2_human Human Yes 6.9 EC50 = 121.9 Funct
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assayAgonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL98836 drd2_rat Rat No 6.9 EC50 = 122 Funct
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
265 2 1 4 2.5 CCCN1CCOC2C1CSC3=C2C=C(C=C3)O
CHEMBL3798179 drd2_human Human No 6.9 EC50 = 124.7 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL1083816 drd2_human Human No 6.9 EC50 = 125.9 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
320 4 0 2 2.9 C1CCCN(CC1)CCN2C=CN(C2=O)C3=CC(=CC=C3)Cl
CHEMBL1084121 drd2_human Human No 6.9 EC50 = 125.9 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
358 4 0 5 2.6 C1CCCN(CC1)CCN2CCN(S2(=O)=O)C3=CC(=CC=C3)Cl
CHEMBL2165126 drd2_human Human Yes 6.9 EC50 = 126 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
462 7 1 4 5.0 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL2165139 drd2_human Human No 6.9 EC50 = 126 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
422 6 0 5 5.6 C1CN(CCN1CCCOC2=CC3=C(C=C2)SC=N3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165130 drd2_human Human No 5.9 EC50 = 1260 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
460 6 1 4 4.1 C1CC(=O)NC2=C1C=CC(=C2)COC3CC3CN4CCN(CC4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3287392 drd2_human Human No 5.9 EC50 = 1288.3 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CN3C(=CC=N3)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1916551 drd2_human Human No 7.9 EC50 = 13 Funct
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
562 18 1 6 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC4=CC=CC=C4C3)OC
CHEMBL3800165 drd2_human Human No 7.9 EC50 = 13 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
273 5 1 2 2.4 CCCNC1CC2=C3C(=CC=C2)N(C(=O)N3C1)CCC
CHEMBL2165119 drd2_human Human Yes 7.9 EC50 = 13 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
463 7 1 5 4.6 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=NC4=C(CCC(=O)N4)C=C3
CHEMBL1916551 drd2_human Human No 7.9 EC50 = 13 Funct
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
562 18 1 6 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC4=CC=CC=C4C3)OC
CHEMBL3099232 drd2_human Human No 7.9 EC50 = 13 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
404 5 1 4 4.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC(=N4)C5=CC=CC=C5
CHEMBL3800165 drd2_human Human No 7.9 EC50 = 13 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
273 5 1 2 2.4 CCCNC1CC2=C3C(=CC=C2)N(C(=O)N3C1)CCC
CHEMBL3298895 drd2_human Human No 7.9 EC50 = 13.2 Funct
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
521 8 2 6 6.4 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)N)C
CHEMBL3298895 drd2_human Human No 7.9 EC50 = 13.2 Funct
Agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayAgonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
521 8 2 6 6.4 CC1=CC(=NC2=C1C(=C(S2)C(=O)NCCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)N)C
CHEMBL468017 drd2_human Human Yes 7.9 EC50 = 13.4 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
468 7 1 6 5.2 CCCN(CCN1CCN(CC1)C2=C(C(=CC=C2)Cl)Cl)C3CCC4=C(C3)SC(=N4)N
CHEMBL468017 drd2_human Human Yes 7.9 EC50 = 13.4 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
468 7 1 6 5.2 CCCN(CCN1CCN(CC1)C2=C(C(=CC=C2)Cl)Cl)C3CCC4=C(C3)SC(=N4)N
CHEMBL569107 drd2_human Human No 7.9 EC50 = 13.5 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
451 7 1 7 4.2 CCCN(CCN1CCN(CC1)C2=CC=CC3=C2C=CC=N3)C4CCC5=C(C4)SC(=N5)N
CHEMBL569107 drd2_human Human No 7.9 EC50 = 13.5 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
451 7 1 7 4.2 CCCN(CCN1CCN(CC1)C2=CC=CC3=C2C=CC=N3)C4CCC5=C(C4)SC(=N5)N
CHEMBL3797209 drd2_human Human No 7.9 EC50 = 13.7 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL3797209 drd2_human Human No 7.9 EC50 = 13.7 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL194493 drd2_human Human No 7.9 EC50 = 13.8 Funct
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
449 6 1 5 4.2 C1CN(CCN1CC=CCNC(=O)C2=CC=C(C=C2)[N+](=O)[O-])C3=C(C(=CC=C3)Cl)Cl
CHEMBL194493 drd2_human Human No 7.9 EC50 = 13.8 Funct
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
449 6 1 5 4.2 C1CN(CCN1CC=CCNC(=O)C2=CC=C(C=C2)[N+](=O)[O-])C3=C(C(=CC=C3)Cl)Cl
CHEMBL372020 drd2_rat Rat No 6.9 EC50 = 130 Funct
Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
245 5 0 2 3.0 CCCN(CCC)C1CCN2C(=CC=C2C#N)C1
CHEMBL2396663 drd2_human Human No 6.9 EC50 = 130 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL372020 drd2_rat Rat No 6.9 EC50 = 130 Funct
Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
245 5 0 2 3.0 CCCN(CCC)C1CCN2C(=CC=C2C#N)C1
CHEMBL2396663 drd2_human Human No 6.9 EC50 = 130 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3287392 drd2_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CN3C(=CC=N3)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2396663 drd2_human Human No 5.9 EC50 = 1300 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3287392 drd2_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CN3C(=CC=N3)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2396663 drd2_human Human No 5.9 EC50 = 1300 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3798748 drd2_human Human No 4.9 EC50 = 13000 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
493 12 4 7 3.5 COC1=C(C=CC(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O)OCCCC4=CC=CC=C4
CHEMBL3798748 drd2_human Human No 4.9 EC50 = 13000 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
493 12 4 7 3.5 COC1=C(C=CC(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O)OCCCC4=CC=CC=C4
CHEMBL3134062 drd2_human Human No 6.9 EC50 = 132 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
366 5 2 4 2.3 CC(=O)NCCCOC1=C(C2=C(CC3C4=C2C=CC=C4CCN3C)C=C1)O
CHEMBL3585372 drd2_human Human No 7.9 EC50 = 14 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
857 37 4 6 11.2 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585372 drd2_human Human No 7.9 EC50 = 14 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
857 37 4 6 11.2 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585372 drd2_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
857 37 4 6 11.2 CCCN(CCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL2397389 drd2_human Human No 6.9 EC50 = 140 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3577344 drd2_human Human No 6.9 EC50 = 140 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL2397389 drd2_human Human No 6.9 EC50 = 140 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3577344 drd2_human Human No 6.9 EC50 = 140 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL3585366 drd2_human Human No 5.9 EC50 = 1413 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
533 17 2 6 4.3 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)N(C2=CC=C1)CCCNC(=O)OC(C)(C)C
CHEMBL3585366 drd2_human Human No 5.9 EC50 = 1413 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
533 17 2 6 4.3 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)N(C2=CC=C1)CCCNC(=O)OC(C)(C)C
CHEMBL3585366 drd2_human Human No 5.8 EC50 = 1445.4 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
533 17 2 6 4.3 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)N(C2=CC=C1)CCCNC(=O)OC(C)(C)C
CHEMBL3394255 drd2_human Human No 6.8 EC50 = 147.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
653 17 4 11 4.0 CCCN(CCCNC(=O)COC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL3394255 drd2_human Human No 6.8 EC50 = 147.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
653 17 4 11 4.0 CCCN(CCCNC(=O)COC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL3394255 drd2_human Human No 6.8 EC50 = 148 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
653 17 4 11 4.0 CCCN(CCCNC(=O)COC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL116372 drd2_rat Rat No 6.8 EC50 = 148 Funct
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay
305 5 1 5 3.9 CCCN(CCC)C1CC2=C(C=CC3=C2SC(=N3)N)OC1
CHEMBL3134065 drd2_human Human No 6.8 EC50 = 149 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
759 15 4 8 5.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL246637 drd2_human Human Yes 7.8 EC50 = 15.3 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
375 3 2 2 4.3 C1CN(CCC1(C2=CC(=C(C=C2)Cl)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL246637 drd2_human Human Yes 7.8 EC50 = 15.3 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
375 3 2 2 4.3 C1CN(CCC1(C2=CC(=C(C=C2)Cl)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL244990 drd2_human Human No 7.8 EC50 = 15.8 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
499 8 2 5 4.4 C1CN(CCN1CC(CCNC(=O)C2=CC=C(C=C2)C3=CC=CC=N3)O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL244990 drd2_human Human No 7.8 EC50 = 15.8 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
499 8 2 5 4.4 C1CN(CCN1CC(CCNC(=O)C2=CC=C(C=C2)C3=CC=CC=N3)O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3125990 drd2_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
492 8 2 7 5.2 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC(=CC=C3)O)C4CCC5=C(C4)SC(=N5)N
CHEMBL231156 drd2_human Human No 6.8 EC50 = 150 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
495 7 1 4 5.3 C1CN(CCN1CC2CC2CNC(=O)C3=CC=C(C=C3)C4=CC=CC=N4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL231156 drd2_human Human No 6.8 EC50 = 150 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
495 7 1 4 5.3 C1CN(CCN1CC2CC2CNC(=O)C3=CC=C(C=C3)C4=CC=CC=N4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL2396663 drd2_human Human No 5.8 EC50 = 1500 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL2396663 drd2_human Human No 5.8 EC50 = 1500 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3798179 drd2_human Human No 6.8 EC50 = 154.5 Funct
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assayAgonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL2057452 drd2_human Human No 4.8 EC50 = 15610 Funct
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL2165123 drd2_human Human No 6.8 EC50 = 158 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
424 9 1 5 3.7 CCOC1=CC=CC(=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL161792 drd2_human Human Yes 6.8 EC50 = 158 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
446 7 1 4 4.9 C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165128 drd2_human Human No 5.8 EC50 = 1580 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
502 6 1 4 5.6 C1CC(CCC1CN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl)COC4=CC5=C(CCC(=O)N5)C=C4
CHEMBL2396663 drd2_human Human No 7.8 EC50 = 16 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL434665 drd2_human Human Yes 7.8 EC50 = 16 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL2396663 drd2_human Human No 7.8 EC50 = 16 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL434665 drd2_human Human Yes 7.8 EC50 = 16 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL346129 drd2_human Human No 7.8 EC50 = 16 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
394 7 1 4 3.7 CC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL310867 drd2_rat Rat Yes 7.8 EC50 = 16 Funct
Effective concentration required for agonistic activity against rat Dopamine receptor D2LEffective concentration required for agonistic activity against rat Dopamine receptor D2L
271 5 0 2 3.6 CCCN(CCC)C1CCC2=NN3C=CC=CC3=C2C1
CHEMBL2165135 drd2_human Human No 7.8 EC50 = 16 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
435 7 2 4 4.1 C1CN(CCN1CCCCOC2=CC3=C(C=C2)NC(=O)N3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3797209 drd2_human Human No 7.8 EC50 = 16.8 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL25856 drd2_human Human No 5.8 EC50 = 1610 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2
267 0 3 3 2.5 C1CC2=CC(=C(C=C2C3C1NCC4=CC=CC=C34)O)O
CHEMBL2057451 drd2_human Human No 4.8 EC50 = 16190 Funct
Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control.
323 2 0 3 4.0 CC1=CC(=C2CN3CCC4=CC(=C(C=C4C3CC2=C1)OC)OC)C
CHEMBL180060 drd2_human Human No 6.8 EC50 = 162 Funct
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D2 receptors expressed in Chinese hamster ovary cells
530 6 1 3 5.0 C1CN(CCN1CC=CCNC(=O)C2=CC=C(C=C2)I)C3=C(C(=CC=C3)Cl)Cl
CHEMBL7549 drd2_human Human No 6.8 EC50 = 163 Funct
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL7549 drd2_human Human No 6.8 EC50 = 163 Funct
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL3800633 drd2_human Human No 6.8 EC50 = 163.3 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL419792 drd2_human Human Yes 6.8 EC50 = 165 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL246855 drd2_human Human Yes 6.8 EC50 = 166 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
425 8 1 2 5.9 CCCCCCN1C=C(C2=CC=CC=C21)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL246855 drd2_human Human Yes 6.8 EC50 = 166 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
425 8 1 2 5.9 CCCCCCN1C=C(C2=CC=CC=C21)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL3799455 drd2_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
473 12 3 5 5.0 COC1=C(C=CC(=C1)CCNCCC2=C3C=CC(=O)NC3=C(C=C2)O)OCCCC4=CC=CC=C4
CHEMBL3799455 drd2_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
473 12 3 5 5.0 COC1=C(C=CC(=C1)CCNCCC2=C3C=CC(=O)NC3=C(C=C2)O)OCCCC4=CC=CC=C4
CHEMBL434665 drd2_human Human Yes 7.8 EC50 = 17.1 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
231 3 2 2 1.3 CCCNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL3797876 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
319 8 4 6 1.6 COC1=CC=CC=C1OCCNCC(C2=CC(=C(C=C2)O)O)O
CHEMBL3597635 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
439 7 1 4 5.1 C1CN(CCN1CCCCNC(=O)C2=CC3=CC=CC=C3N=C2)C4=CC=CC5=CC=CC=C54
CHEMBL1627305 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
461 7 3 4 4.3 C1CN(CCN1CC(CCNC(=O)C2=CC3=CC=CC=C3N2)O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3797876 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
319 8 4 6 1.6 COC1=CC=CC=C1OCCNCC(C2=CC(=C(C=C2)O)O)O
CHEMBL3597635 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
439 7 1 4 5.1 C1CN(CCN1CCCCNC(=O)C2=CC3=CC=CC=C3N=C2)C4=CC=CC5=CC=CC=C54
CHEMBL1627305 drd2_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
461 7 3 4 4.3 C1CN(CCN1CC(CCNC(=O)C2=CC3=CC=CC=C3N2)O)C4=C(C(=CC=C4)Cl)Cl
CHEMBL132575 drd2_human Human No 6.8 EC50 = 170 Funct
Tested for intrinsic activity towards Dopamine receptor D2 in CHO cellsTested for intrinsic activity towards Dopamine receptor D2 in CHO cells
264 5 1 3 3.3 CCCN(CCC)C1CCC2=C(C1)CCCC2=NO
CHEMBL3577344 drd2_human Human No 5.8 EC50 = 1700 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL3577344 drd2_human Human No 5.8 EC50 = 1700 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL3287390 drd2_human Human No 6.8 EC50 = 177.8 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CC3=CC=NN3C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2387709 drd2_human Human No 6.8 EC50 = 179 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
393 7 1 4 4.5 CCCN(CCN1CCN(CC1)C2=CC=CC=C2)C3CCC4=C(C3)C=C(C=C4)N
CHEMBL2165133 drd2_human Human No 7.8 EC50 = 18 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
448 7 1 4 4.8 C1CNC(=O)C2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3797740 drd2_human Human No 7.7 EC50 = 18.1 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
245 3 1 2 1.8 CCCN(C)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL3797740 drd2_human Human No 7.7 EC50 = 18.1 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
245 3 1 2 1.8 CCCN(C)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL118636 drd2_rat Rat No 7.7 EC50 = 18.7 Funct
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
289 5 1 4 4.2 CCCN(CCC)C1CC2=C(C1)C3=C(C=C2)N=C(S3)N
CHEMBL3287390 drd2_human Human No 6.8 EC50 = 180 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CC3=CC=NN3C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287390 drd2_human Human No 6.8 EC50 = 180 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
419 7 0 4 4.6 C1CN(CCN1CCCCOC2=CC3=CC=NN3C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2180638 drd2_human Human Yes 6.7 EC50 = 181 Funct
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
295 8 1 2 4.6 C1CC1CN(CCC2=CC=CC=C2)CCC3=CC(=CC=C3)O
CHEMBL3613875 drd2_human Human No 5.7 EC50 = 1862.1 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
498 8 0 6 3.8 C1CN(CCN1CCCCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613875 drd2_human Human No 5.7 EC50 = 1862.1 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
498 8 0 6 3.8 C1CN(CCN1CCCCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL7549 drd2_rat Rat No 7.7 EC50 = 19 Funct
Effective concentration required for agonistic activity against rat D2 long receptorEffective concentration required for agonistic activity against rat D2 long receptor
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL7549 drd2_rat Rat No 7.7 EC50 = 19 Funct
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL3800633 drd2_human Human No 7.7 EC50 = 19.5 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3800633 drd2_human Human No 7.7 EC50 = 19.5 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL514885 drd2_human Human Yes 7.7 EC50 = 19.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL467540 drd2_human Human No 7.7 EC50 = 19.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL514885 drd2_human Human Yes 7.7 EC50 = 19.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL467540 drd2_human Human No 7.7 EC50 = 19.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL3613874 drd2_human Human No 6.7 EC50 = 190.6 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
484 7 0 6 3.5 C1CN(CCN1CCCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613874 drd2_human Human No 6.7 EC50 = 190.6 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
484 7 0 6 3.5 C1CN(CCN1CCCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3577343 drd2_human Human No 5.7 EC50 = 1900 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3577343 drd2_human Human No 5.7 EC50 = 1900 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL87734 drd2_rat Rat No 6.7 EC50 = 192 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
287 2 4 5 1.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC(=CC=C3)O
CHEMBL2165129 drd2_human Human No 6.7 EC50 = 199 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
444 4 1 4 4.0 C1CC(=O)NC2=C1C=CC(=C2)OCC#CCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3613876 drd2_human Human No 6.7 EC50 = 199.5 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
470 6 0 6 3.1 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613876 drd2_human Human No 6.7 EC50 = 199.5 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
470 6 0 6 3.1 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL155731 drd2_human Human Yes 8.7 EC50 = 2 Funct
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL2165121 drd2_human Human No 8.7 EC50 = 2 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
438 9 1 5 4.2 CC(C)OC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL157923 drd2_human Human No 8.7 EC50 = 2 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
414 7 1 4 4.0 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4Cl
CHEMBL2165125 drd2_human Human No 8.7 EC50 = 2 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
447 7 1 3 5.3 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL155731 drd2_human Human Yes 8.7 EC50 = 2 Funct
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL2165126 drd2_human Human Yes 8.7 EC50 = 2 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
462 7 1 4 5.0 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3577346 drd2_human Human No 8.7 EC50 = 2.1 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL3577346 drd2_human Human No 8.7 EC50 = 2.1 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL246439 drd2_human Human Yes 8.7 EC50 = 2.1 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 2 2 4.1 CC1=C(C2=CC=CC=C2N1)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL246439 drd2_human Human Yes 8.7 EC50 = 2.1 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 2 2 4.1 CC1=C(C2=CC=CC=C2N1)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL250552 drd2_human Human No 8.7 EC50 = 2.2 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
394 7 1 4 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2)C3CCC4=C(C3)C=CC=C4O
CHEMBL250552 drd2_human Human No 8.7 EC50 = 2.2 Funct
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
394 7 1 4 4.8 CCCN(CCN1CCN(CC1)C2=CC=CC=C2)C3CCC4=C(C3)C=CC=C4O
CHEMBL2165122 drd2_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
448 7 1 7 4.3 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4C(F)(F)F
CHEMBL2165120 drd2_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
460 7 1 4 5.3 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)C=CC(=O)N4
CHEMBL160296 drd2_human Human No 8.6 EC50 = 2.5 Funct
Partial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayPartial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
410 8 1 5 3.4 COC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL1079190 drd2_human Human No 8.6 EC50 = 2.5 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
308 3 0 2 2.6 CN1CCCCC1CN2CCN(C2=O)C3=CC(=CC=C3)Cl
CHEMBL26181 drd2_human Human Yes 8.6 EC50 = 2.5 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
273 5 1 2 2.7 CCCN(CCC)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL26181 drd2_human Human Yes 8.6 EC50 = 2.5 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
273 5 1 2 2.7 CCCN(CCC)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL3800341 drd2_human Human No 8.6 EC50 = 2.6 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
477 12 3 6 4.6 COC1=C(C=CC(=C1)CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)OCCCC4=CC=CC=C4
CHEMBL3800341 drd2_human Human No 8.6 EC50 = 2.6 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
477 12 3 6 4.6 COC1=C(C=CC(=C1)CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)OCCCC4=CC=CC=C4
CHEMBL3298827 drd2_human Human No 8.6 EC50 = 2.7 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
532 10 2 8 5.7 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCN3CCN(CC3)C4=CC=CC=C4OC)N
CHEMBL3298827 drd2_human Human No 8.6 EC50 = 2.7 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
532 10 2 8 5.7 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCN3CCN(CC3)C4=CC=CC=C4OC)N
CHEMBL3298827 drd2_human Human No 8.6 EC50 = 2.7 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
532 10 2 8 5.7 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCN3CCN(CC3)C4=CC=CC=C4OC)N
CHEMBL2165120 drd2_human Human No 8.6 EC50 = 2.8 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
460 7 1 4 5.3 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)C=CC(=O)N4
CHEMBL423499 drd2_human Human No 8.6 EC50 = 2.8 Funct
Inhibition of [3H]thymidine uptake by Dopamine receptor D2Inhibition of [3H]thymidine uptake by Dopamine receptor D2
389 5 1 3 5.5 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=N3)C4=CNC5=CC=CC=C54
CHEMBL86801 drd2_human Human No 8.6 EC50 = 2.8 Funct
Inhibition of [3H]thymidine uptake by Dopamine receptor D2Inhibition of [3H]thymidine uptake by Dopamine receptor D2
389 5 1 3 5.5 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=N3)C4=CNC5=CC=CC=C54
CHEMBL3577346 drd2_human Human No 8.5 EC50 = 2.9 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL3577346 drd2_human Human No 8.5 EC50 = 2.9 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL2152633 drd2_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
439 7 2 6 4.1 CCCN(CCN1CCN(CC1)C2=CC3=C(C=C2)NC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL2152633 drd2_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
439 7 2 6 4.1 CCCN(CCN1CCN(CC1)C2=CC3=C(C=C2)NC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL53 drd2_human Human Yes 7.7 EC50 = 20 Funct
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL400827 drd2_human Human Yes 7.7 EC50 = 20 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 1 2 3.6 CN1C=C(C2=CC=CC=C21)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL2165117 drd2_human Human No 7.7 EC50 = 20 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
434 6 1 4 4.4 C1CNC(=O)C2=C1C=CC(=C2)OCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165115 drd2_human Human No 7.7 EC50 = 20 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
434 7 2 3 4.8 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)NC(=O)N4
CHEMBL53 drd2_human Human Yes 7.7 EC50 = 20 Funct
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL400827 drd2_human Human Yes 7.7 EC50 = 20 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 1 2 3.6 CN1C=C(C2=CC=CC=C21)CN3CCC(CC3)(C4=CC=C(C=C4)Cl)O
CHEMBL3797209 drd2_human Human No 7.7 EC50 = 20.5 Funct
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assayAgonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL3800303 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
438 12 4 6 4.1 COC1=C(C=CC(=C1)CCNCC(C2=CC(=C(C=C2)O)O)O)OCCCC3=CC=CC=C3
CHEMBL3597636 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
455 7 2 5 4.1 C1CN(CCN1CC(CCNC(=O)C2=CC3=CC=CC=C3N=C2)O)C4=CC=CC5=CC=CC=C54
CHEMBL2165116 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
405 6 1 4 4.8 C1CN(CCN1CCCOC2=CC3=C(C=C2)C=NN3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL160744 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
408 7 1 4 4.1 CC1=C(C(=CC=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3)C
CHEMBL3800303 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
438 12 4 6 4.1 COC1=C(C=CC(=C1)CCNCC(C2=CC(=C(C=C2)O)O)O)OCCCC3=CC=CC=C3
CHEMBL3597636 drd2_human Human No 6.7 EC50 = 200 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
455 7 2 5 4.1 C1CN(CCN1CC(CCNC(=O)C2=CC3=CC=CC=C3N=C2)O)C4=CC=CC5=CC=CC=C54
CHEMBL86325 drd2_rat Rat No 6.7 EC50 = 204 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
315 5 3 5 1.4 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)COCC3=CC=CC=C3
CHEMBL3800633 drd2_human Human No 6.7 EC50 = 209.9 Funct
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assayAgonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL2165137 drd2_human Human No 7.7 EC50 = 21 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
435 7 0 4 6.6 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)SC=N4
CHEMBL2165128 drd2_human Human No 5.7 EC50 = 2100 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
502 6 1 4 5.6 C1CC(CCC1CN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl)COC4=CC5=C(CCC(=O)N5)C=C4
CHEMBL398368 drd2_human Human No 6.7 EC50 = 216 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
407 9 2 3 5.3 CCCCCCOC1=CC=C(C=C1)C2(CCN(CC2)CC3=CNC4=CC=CC=C43)O
CHEMBL398368 drd2_human Human No 6.7 EC50 = 216 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
407 9 2 3 5.3 CCCCCCOC1=CC=C(C=C1)C2(CCN(CC2)CC3=CNC4=CC=CC=C43)O
CHEMBL3585365 drd2_human Human No 6.7 EC50 = 218.8 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
376 11 2 4 2.9 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3585365 drd2_human Human No 6.7 EC50 = 219 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
376 11 2 4 2.9 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3585365 drd2_human Human No 6.7 EC50 = 219 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
376 11 2 4 2.9 CCCN(CCCNC(=O)OC(C)(C)C)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3585369 drd2_human Human No 7.7 EC50 = 22 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
689 25 4 6 4.7 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585369 drd2_human Human No 7.7 EC50 = 22 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
689 25 4 6 4.7 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585369 drd2_human Human No 7.7 EC50 = 22.4 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
689 25 4 6 4.7 CCCN(CCCNC(=O)CCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3798179 drd2_human Human No 7.6 EC50 = 22.7 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3798179 drd2_human Human No 7.6 EC50 = 22.7 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3134069 drd2_human Human No 6.7 EC50 = 224 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
871 23 4 8 10.2 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCCCCCCCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL246230 drd2_human Human No 6.7 EC50 = 225 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
350 3 1 2 4.2 C1CN(CCC1(C#N)C2=CC=C(C=C2)Cl)CC3=CNC4=CC=CC=C43
CHEMBL246230 drd2_human Human No 6.7 EC50 = 225 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
350 3 1 2 4.2 C1CN(CCC1(C#N)C2=CC=C(C=C2)Cl)CC3=CNC4=CC=CC=C43
CHEMBL465054 drd2_rat Rat No 7.6 EC50 = 23 Funct
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
343 1 2 3 3.9 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5
CHEMBL2165114 drd2_human Human No 7.6 EC50 = 23 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
450 7 0 5 6.3 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)SC=N4
CHEMBL465054 drd2_rat Rat No 7.6 EC50 = 23 Funct
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
343 1 2 3 3.9 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5
CHEMBL244774 drd2_human Human No 6.6 EC50 = 231 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
497 7 1 4 4.0 C1CN(CCN1CC=CCNC(=O)C2=CC=C(C=C2)C3=CC=CC=[N+]3[O-])C4=C(C(=CC=C4)Cl)Cl
CHEMBL244774 drd2_human Human No 6.6 EC50 = 231 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
497 7 1 4 4.0 C1CN(CCN1CC=CCNC(=O)C2=CC=C(C=C2)C3=CC=CC=[N+]3[O-])C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287403 drd2_human Human No 6.6 EC50 = 234.4 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
462 8 1 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=NO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL246021 drd2_human Human No 7.6 EC50 = 24.8 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
382 4 2 2 3.7 CC(=O)NC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL246021 drd2_human Human No 7.6 EC50 = 24.8 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
382 4 2 2 3.7 CC(=O)NC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL3799455 drd2_human Human No 6.6 EC50 = 240 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
473 12 3 5 5.0 COC1=C(C=CC(=C1)CCNCCC2=C3C=CC(=O)NC3=C(C=C2)O)OCCCC4=CC=CC=C4
CHEMBL3287403 drd2_human Human No 6.6 EC50 = 240 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
462 8 1 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=NO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3799455 drd2_human Human No 6.6 EC50 = 240 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
473 12 3 5 5.0 COC1=C(C=CC(=C1)CCNCCC2=C3C=CC(=O)NC3=C(C=C2)O)OCCCC4=CC=CC=C4
CHEMBL3287403 drd2_human Human No 6.6 EC50 = 240 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
462 8 1 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=NO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2112745 drd2_human Human No 6.6 EC50 = 240 Funct
In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptorIn vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor
419 4 1 4 4.4 C1CC(CC2C1CC(CC2)N3CCN(CC3)C4=CC=CC=N4)NC(=O)C5=CC=CC=C5
CHEMBL2397389 drd2_human Human No 5.6 EC50 = 2400 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL2397389 drd2_human Human No 5.6 EC50 = 2400 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL3134071 drd2_human Human No 6.6 EC50 = 248 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
955 29 4 8 13.5 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL3797758 drd2_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
303 8 3 5 2.7 COC1=CC=CC=C1OCCNCCC2=CC(=C(C=C2)O)O
CHEMBL2165115 drd2_human Human No 7.6 EC50 = 25 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
434 7 2 3 4.8 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)NC(=O)N4
CHEMBL378455 drd2_human Human No 7.6 EC50 = 25 Funct
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL2165114 drd2_human Human No 7.6 EC50 = 25 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
450 7 0 5 6.3 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(C=C3)SC=N4
CHEMBL2165122 drd2_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
448 7 1 7 4.3 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4C(F)(F)F
CHEMBL2165121 drd2_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
438 9 1 5 4.2 CC(C)OC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3797758 drd2_human Human No 7.6 EC50 = 25 Funct
Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
303 8 3 5 2.7 COC1=CC=CC=C1OCCNCCC2=CC(=C(C=C2)O)O
CHEMBL378455 drd2_human Human No 7.6 EC50 = 25 Funct
Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL225230 drd2_human Human Yes 7.6 EC50 = 25.1 Funct
Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayActivity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
295 2 2 3 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL225230 drd2_human Human Yes 7.6 EC50 = 25.1 Funct
Activity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayActivity at human dopamine D2 receptor in NIH/3T3 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
295 2 2 3 3.2 CCCN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL2165127 drd2_human Human No 6.6 EC50 = 251 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
434 6 1 4 4.3 C1CC(=O)NC2=C1C=CC(=C2)OCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165124 drd2_human Human No 6.6 EC50 = 251 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
424 9 1 5 3.7 CCOC1=CC=C(C=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL1945039 drd2_human Human No 6.6 EC50 = 251.2 Funct
Binding affinity to dopamine D2 receptor expressed in HEK cells by GTPgammaS binding assayBinding affinity to dopamine D2 receptor expressed in HEK cells by GTPgammaS binding assay
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945039 drd2_human Human No 6.6 EC50 = 251.2 Funct
Binding affinity to dopamine D2 receptor expressed in HEK cells by GTPgammaS binding assayBinding affinity to dopamine D2 receptor expressed in HEK cells by GTPgammaS binding assay
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1765633 drd2_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL1765633 drd2_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL393027 drd2_human Human Yes 6.6 EC50 = 260 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 2 2 4.0 C1CC(CCN(C1)CC2=CNC3=CC=CC=C32)(C4=CC=C(C=C4)Cl)O
CHEMBL393027 drd2_human Human Yes 6.6 EC50 = 260 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 3 2 2 4.0 C1CC(CCN(C1)CC2=CNC3=CC=CC=C32)(C4=CC=C(C=C4)Cl)O
CHEMBL3800636 drd2_human Human No 5.6 EC50 = 2600 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
422 12 3 5 5.3 COC1=C(C=CC(=C1)CCNCCC2=CC(=C(C=C2)O)O)OCCCC3=CC=CC=C3
CHEMBL3800636 drd2_human Human No 5.6 EC50 = 2600 Funct
Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assayAgonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay
422 12 3 5 5.3 COC1=C(C=CC(=C1)CCNCCC2=CC(=C(C=C2)O)O)OCCCC3=CC=CC=C3
CHEMBL3134063 drd2_human Human No 6.6 EC50 = 266 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
538 13 3 6 4.0 CC(C)(C)OC(=O)NCCCCCC(=O)NCCCOC1=C(C2=C(CC3C4=C2C=CC=C4CCN3C)C=C1)O
CHEMBL484598 drd2_human Human No 6.6 EC50 = 269.2 Funct
Activation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
286 2 1 3 1.6 CCCN1CCOC2C1CCC3=C2C=C4C(=C3)CNC4=O
CHEMBL484598 drd2_human Human No 6.6 EC50 = 269.2 Funct
Activation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
286 2 1 3 1.6 CCCN1CCOC2C1CCC3=C2C=C4C(=C3)CNC4=O
CHEMBL3798179 drd2_human Human No 7.6 EC50 = 27.7 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3798179 drd2_human Human No 7.6 EC50 = 27.7 Funct
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
418 7 3 3 3.0 CN(CCCCNC(=O)C1=CC2=CC=CC=C2N1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3287403 drd2_human Human No 6.6 EC50 = 270 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
462 8 1 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=NO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165126 drd2_human Human Yes 6.6 EC50 = 270 Funct
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assayPartial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
462 7 1 4 5.0 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL3287403 drd2_human Human No 6.6 EC50 = 275.4 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
462 8 1 6 4.4 C1CN(CCN1CCCCOC2=CC3=C(C=NN3C=C2)C=NO)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3585368 drd2_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
633 21 4 6 2.9 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3577342 drd2_human Human No 7.6 EC50 = 28 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3585368 drd2_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
633 21 4 6 2.9 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3577342 drd2_human Human No 7.6 EC50 = 28 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL355371 drd2_human Human No 7.6 EC50 = 28 Funct
The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2
367 6 1 6 3.3 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=N3)NC4=NC=CC=N4
CHEMBL3585368 drd2_human Human No 7.6 EC50 = 28.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
633 21 4 6 2.9 CCCN(CCCNC(=O)CCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL83080 drd2_rat Rat Yes 5.6 EC50 = 2850 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL315849 drd2_rat Rat No 6.5 EC50 = 286 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
233 2 3 4 0.6 C#CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3797740 drd2_human Human No 7.5 EC50 = 29 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 2 1.8 CCCN(C)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL3797740 drd2_human Human No 7.5 EC50 = 29 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 2 1.8 CCCN(C)C1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL165679 drd2_human Human No 7.5 EC50 = 29 Funct
The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2
366 6 1 5 4.0 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=C3)NC4=NC=CC=N4
CHEMBL3084971 drd2_human Human No 7.5 EC50 = 29 Funct
The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2The in vitro intrinsic activity was measured at DA D2 receptor by measuring its ability to increase [3H]thymidine uptake in CHO-K1 cells transfected with the Dopamine receptor D2
366 6 1 5 4.0 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=C3)NC4=NC=CC=N4
CHEMBL3577343 drd2_human Human No 5.5 EC50 = 2900 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3577343 drd2_human Human No 5.5 EC50 = 2900 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL378455 drd2_human Human No 8.5 EC50 = 3 Funct
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL378455 drd2_human Human No 8.5 EC50 = 3 Funct
Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL3577346 drd2_human Human No 8.5 EC50 = 3.1 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL3577346 drd2_human Human No 8.5 EC50 = 3.1 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL1303 drd2_human Human Yes 8.5 EC50 = 3.2 Funct
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
316 6 1 3 4.9 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
CHEMBL1774063 drd2_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
449 7 1 5 4.2 C1CC(=O)NC2=C1C=CC(=N2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL346129 drd2_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
394 7 1 4 3.7 CC1=CC=CC=C1N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL2165119 drd2_human Human Yes 8.5 EC50 = 3.3 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
463 7 1 5 4.6 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=NC4=C(CCC(=O)N4)C=C3
CHEMBL2165126 drd2_human Human Yes 8.5 EC50 = 3.3 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
462 7 1 4 5.0 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL2028019 drd2_human Human Yes 8.5 EC50 = 3.5 Funct
Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assayPartial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3085826 drd2_human Human Yes 8.5 EC50 = 3.5 Funct
Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assayPartial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL2028019 drd2_human Human Yes 8.5 EC50 = 3.5 Funct
Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assayPartial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3085826 drd2_human Human Yes 8.5 EC50 = 3.5 Funct
Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assayPartial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
427 5 1 3 4.3 CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3099239 drd2_human Human No 8.5 EC50 = 3.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
362 4 1 4 3.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=C(C=N4)Cl
CHEMBL3585370 drd2_human Human No 8.4 EC50 = 3.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
745 29 4 6 6.9 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585370 drd2_human Human No 8.4 EC50 = 3.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
745 29 4 6 6.9 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3585370 drd2_human Human No 8.4 EC50 = 3.9 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
745 29 4 6 6.9 CCCN(CCCNC(=O)CCCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1)CCC3=C4CC(=O)NC4=CC=C3
CHEMBL3577345 drd2_human Human No 7.5 EC50 = 30 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL53 drd2_rat Rat Yes 7.5 EC50 = 30 Funct
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL2165117 drd2_human Human No 7.5 EC50 = 30 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
434 6 1 4 4.4 C1CNC(=O)C2=C1C=CC(=C2)OCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL589 drd2_human Human Yes 7.5 EC50 = 30 Funct
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assayPartial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3577345 drd2_human Human No 7.5 EC50 = 30 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL53 drd2_rat Rat Yes 7.5 EC50 = 30 Funct
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counterAgonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL3798803 drd2_human Human No 7.5 EC50 = 30.5 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
259 4 1 2 1.9 CCCCN1C2=CC=CC3=C2N(C1=O)CC(C3)NC
CHEMBL3798803 drd2_human Human No 7.5 EC50 = 30.5 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
259 4 1 2 1.9 CCCCN1C2=CC=CC3=C2N(C1=O)CC(C3)NC
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 302 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 302 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 304 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL442926 drd2_rat Rat Yes 6.5 EC50 = 308 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
593 5 4 8 4.8 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OCCOC5=CC6=C7C(CC8=C(C7=C5)C(=C(C=C8)O)O)N(CC6)C)C(=C(C=C4)O)O
CHEMBL442926 drd2_rat Rat Yes 6.5 EC50 = 308 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
593 5 4 8 4.8 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OCCOC5=CC6=C7C(CC8=C(C7=C5)C(=C(C=C8)O)O)N(CC6)C)C(=C(C=C4)O)O
CHEMBL246020 drd2_human Human No 6.5 EC50 = 314 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
339 3 1 1 5.3 CC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL246020 drd2_human Human No 6.5 EC50 = 314 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
339 3 1 1 5.3 CC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL457275 drd2_rat Rat Yes 6.5 EC50 = 315 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
327 3 3 5 1.6 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OCCO)C(=C(C=C4)O)O
CHEMBL457275 drd2_rat Rat Yes 6.5 EC50 = 315 Funct
Agonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at rat dopamine D2(short) receptor expressed in CHOK1 cells by [35S]GTPgammaS binding assay
327 3 3 5 1.6 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OCCO)C(=C(C=C4)O)O
CHEMBL2165131 drd2_human Human No 6.5 EC50 = 316 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
482 5 1 4 5.3 C1CC(=O)NC2=C1C=CC(=C2)OC3=CC=CC(=C3)CN4CCN(CC4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL378455 drd2_human Human No 7.5 EC50 = 32 Funct
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL378455 drd2_human Human No 7.5 EC50 = 32 Funct
Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay
315 4 0 2 3.6 C1CN(CC=C1C2=CC=CC=C2)CC3=CN(N=C3)C4=CC=CC=C4
CHEMBL419792 drd2_human Human Yes 7.5 EC50 = 32.2 Funct
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assayAgonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL1806874 drd2_human Human No 6.5 EC50 = 320 Funct
Agonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
468 9 0 5 6.0 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC(=O)CCCCC5CCSS5
CHEMBL1806874 drd2_human Human No 6.5 EC50 = 320 Funct
Agonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at dopamine D2 receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
468 9 0 5 6.0 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC(=O)CCCCC5CCSS5
CHEMBL3099233 drd2_human Human No 7.5 EC50 = 33 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 minsAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
404 5 1 4 4.2 CCCN1CC(OC2C1CC3=C(C2)C(=CC=C3)O)CN4C=CC(=N4)C5=CC=CC=C5
CHEMBL514885 drd2_human Human Yes 7.5 EC50 = 33.1 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL514885 drd2_human Human Yes 7.5 EC50 = 33.1 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
476 8 1 6 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)SC(=N5)N
CHEMBL3797209 drd2_human Human No 7.5 EC50 = 33.9 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL3797209 drd2_human Human No 7.5 EC50 = 33.9 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
315 7 0 2 3.7 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)N(CCC)CCC
CHEMBL589 drd2_human Human Yes 6.5 EC50 = 330 Funct
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
260 7 1 2 2.7 CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3287399 drd2_human Human No 6.5 EC50 = 338.8 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
447 8 0 5 4.1 C1CN(CCN1CCCCOC2=CN3C(=C(C=N3)C=O)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL397770 drd2_human Human Yes 7.5 EC50 = 34.3 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
375 3 2 2 4.3 C1CN(CCC1(C2=C(C(=CC=C2)Cl)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL397770 drd2_human Human Yes 7.5 EC50 = 34.3 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
375 3 2 2 4.3 C1CN(CCC1(C2=C(C(=CC=C2)Cl)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL246438 drd2_human Human No 7.5 EC50 = 34.7 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 4 1 2 4.2 COC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL246438 drd2_human Human No 7.5 EC50 = 34.7 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
355 4 1 2 4.2 COC1(CCN(CC1)CC2=CNC3=CC=CC=C32)C4=CC=C(C=C4)Cl
CHEMBL3287399 drd2_human Human No 6.5 EC50 = 340 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
447 8 0 5 4.1 C1CN(CCN1CCCCOC2=CN3C(=C(C=N3)C=O)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3287399 drd2_human Human No 6.5 EC50 = 340 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
447 8 0 5 4.1 C1CN(CCN1CCCCOC2=CN3C(=C(C=N3)C=O)C=C2)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165140 drd2_human Human No 6.5 EC50 = 348 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
436 6 0 5 5.9 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCOC3=CC4=C(C=C3)SC=N4
CHEMBL419792 drd2_rat Rat Yes 7.5 EC50 = 35 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL3613876 drd2_human Human No 5.5 EC50 = 3548.1 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
470 6 0 6 3.1 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3613876 drd2_human Human No 5.5 EC50 = 3548.1 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
470 6 0 6 3.1 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=C(C=NN4C=C3)C=O)C5=C(C(=CC=C5)Cl)Cl
CHEMBL415080 drd2_rat Rat No 6.5 EC50 = 358 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
350 2 3 4 2.2 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=C(C=C3)Br
CHEMBL431220 drd2_rat Rat No 6.5 EC50 = 359 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
251 4 3 4 1.8 CCCCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3125987 drd2_human Human No 7.4 EC50 = 36.8 Funct
Partial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingPartial agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
506 9 1 7 5.6 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC(=CC=C3)OC)C4CCC5=C(C4)SC(=N5)N
CHEMBL2165125 drd2_human Human No 6.4 EC50 = 363 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
447 7 1 3 5.3 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL209645 drd2_human Human No 6.4 EC50 = 366 Funct
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assayAgonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
356 7 0 6 3.9 CON=C(CCCN1CCN(CC1)C2=CC=CC=N2)C3=CC=C(C=C3)F
CHEMBL209645 drd2_human Human No 6.4 EC50 = 366 Funct
Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assayAgonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay
356 7 0 6 3.9 CON=C(CCCN1CCN(CC1)C2=CC=CC=N2)C3=CC=C(C=C3)F
CHEMBL3394266 drd2_human Human No 7.4 EC50 = 37.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
518 14 3 9 3.8 CCCN(CCCCCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL3799603 drd2_human Human No 7.4 EC50 = 37.6 Funct
Agonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysisAgonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysis
422 8 1 4 5.1 C1CN(CCN1CCCCNC(=O)OC2=CC=CC=C2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL3799603 drd2_human Human No 7.4 EC50 = 37.6 Funct
Agonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysisAgonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysis
422 8 1 4 5.1 C1CN(CCN1CCCCNC(=O)OC2=CC=CC=C2)C3=C(C(=CC=C3)Cl)Cl
CHEMBL1765633 drd2_human Human No 6.4 EC50 = 370 Funct
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation counting
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL1765633 drd2_human Human No 6.4 EC50 = 370 Funct
Agonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation countingAgonist activity at human dopamine D2long receptor expressed in HEK293 cells co-expressing Galphai2 assessed as incorporation of [35S]GTPgammaS into Galphai2 after 30 mins by scintillation counting
431 10 1 3 4.9 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCN4C(=CC=N4)C3
CHEMBL2165133 drd2_human Human No 5.4 EC50 = 3700 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
448 7 1 4 4.8 C1CNC(=O)C2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL7549 drd2_human Human No 6.4 EC50 = 376 Funct
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL7549 drd2_human Human No 6.4 EC50 = 376 Funct
Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM)
219 3 1 2 3.0 CCCN1CCCC(C1)C2=CC(=CC=C2)O
CHEMBL3394266 drd2_human Human No 7.4 EC50 = 38 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
518 14 3 9 3.8 CCCN(CCCCCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL3394266 drd2_human Human No 7.4 EC50 = 38 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
518 14 3 9 3.8 CCCN(CCCCCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL3799157 drd2_human Human No 7.4 EC50 = 38.7 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 2 1.5 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)NC
CHEMBL3799157 drd2_human Human No 7.4 EC50 = 38.7 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
245 3 1 2 1.5 CCCN1C2=CC=CC3=C2N(C1=O)CC(C3)NC
CHEMBL3577342 drd2_human Human No 6.4 EC50 = 380 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL1916548 drd2_human Human No 6.4 EC50 = 380 Funct
Partial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayPartial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
1053 34 1 13 10.5 CCCN(CCCCNC(=O)C1=CC(=C(C=C1)OCCCC2=CN(N=N2)CCCCCCCCN3C=C(N=N3)CCCOC4=C(C=C(C=C4)CN5CCN(CC5)C6=CC=CC=C6OC)OC)OC)C7CC8=CC=CC=C8C7
CHEMBL3577342 drd2_human Human No 6.4 EC50 = 380 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL1916548 drd2_human Human No 6.4 EC50 = 380 Funct
Partial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayPartial agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
1053 34 1 13 10.5 CCCN(CCCCNC(=O)C1=CC(=C(C=C1)OCCCC2=CN(N=N2)CCCCCCCCN3C=C(N=N3)CCCOC4=C(C=C(C=C4)CN5CCN(CC5)C6=CC=CC=C6OC)OC)OC)C7CC8=CC=CC=C8C7
CHEMBL3577344 drd2_human Human No 5.4 EC50 = 3800 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL3577344 drd2_human Human No 5.4 EC50 = 3800 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
633 20 3 8 5.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)CCC3=C4C=CC(=O)NC4=C(C=C3)O)OC
CHEMBL3134070 drd2_human Human No 6.4 EC50 = 385 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
927 27 4 8 12.4 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCCCCCCCCCCCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL3394264 drd2_human Human No 6.4 EC50 = 389 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
448 9 3 9 1.8 CN(CCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL3394264 drd2_human Human No 6.4 EC50 = 389 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
448 9 3 9 1.8 CN(CCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL3394264 drd2_human Human No 6.4 EC50 = 389.1 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
448 9 3 9 1.8 CN(CCCNC1=NC2=NC(=NN2C(=N1)N)C3=CC=CO3)CCC4=C5CC(=O)NC5=CC=C4
CHEMBL1188090 drd2_human Human Yes 7.4 EC50 = 39 Funct
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assayAgonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
283 8 1 2 4.7 CCCN(CCC1=CC=CC=C1)CCC2=CC(=CC=C2)O
CHEMBL28338 drd2_human Human Yes 5.4 EC50 = 3900 Funct
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2
315 2 3 4 3.4 CCCC1=CC2=C(S1)CNC3C2C4=CC(=C(C=C4CC3)O)O
CHEMBL315468 drd2_rat Rat No 5.4 EC50 = 3910 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
271 2 3 4 1.5 C1C(OC(C2=C1C(=C(C=C2)O)O)CN)C3=CC=CC=C3
CHEMBL3134064 drd2_human Human No 6.4 EC50 = 396 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
731 13 4 8 5.2 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL2165132 drd2_human Human No 6.4 EC50 = 399 Funct
Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).Beta-Arrestin Recruitment (Tango) Assay: Recruitment of β-arrestin to agonist-stimulated D2 receptors was performed using a previously described Tango-type assay (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). Briefly, HTLA cells stably expressing β-arrestin-TEV protease and a tetracycline transactivator-driven luciferase were plated in 15-cm dishes in DMEM containing 10% fetal bovine serum and transfected (via calcium phosphate) with 20 μg of a D2V2-TCS-tTA construct (Barnea et al., Proc. Natl. Acad. Sci. USA 105:64 (2008)). The next day, cells were plated in white, clear-bottom, 384-well plates (Greiner, 10,000 cells/well, 50 μl/well) in DMEM containing 1% dialyzed fetal bovine serum. The following day, the cells were challenged with 10 μl/well of reference agonist (6 μM) or D2 test ligand (6 μM)±reference agonist prepared in HBS, 20 mM HEPES, pH 7.4, 18% DMSO (final ligand concentrations were 1 μM, final DMSO concentration was 3%).
482 5 1 4 5.3 C1CC(=O)NC2=C1C=CC(=C2)OC3=CC=C(C=C3)CN4CCN(CC4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL53 drd2_human Human Yes 8.4 EC50 = 4 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL3577346 drd2_human Human No 8.4 EC50 = 4 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL53 drd2_human Human Yes 8.4 EC50 = 4 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_human Human Yes 8.4 EC50 = 4 Funct
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 minsAgonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL3577346 drd2_human Human No 8.4 EC50 = 4 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
592 18 2 7 6.1 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CCC4=C(C3)C=CC=C4O)OC
CHEMBL2165133 drd2_human Human No 8.4 EC50 = 4 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
448 7 1 4 4.8 C1CNC(=O)C2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1303 drd2_human Human Yes 8.4 EC50 = 4.1 Funct
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assayPartial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
316 6 1 3 4.9 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
CHEMBL1303 drd2_human Human Yes 8.4 EC50 = 4.4 Funct
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assayPartial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
316 6 1 3 4.9 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
CHEMBL445102 drd2_human Human Yes 8.4 EC50 = 4.5 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
341 3 2 2 3.7 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL445102 drd2_human Human Yes 8.4 EC50 = 4.5 Funct
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
341 3 2 2 3.7 C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CC3=CNC4=CC=CC=C43
CHEMBL82663 drd2_human Human Yes 8.4 EC50 = 4.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assayAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL82663 drd2_human Human Yes 8.4 EC50 = 4.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assayAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL599636 drd2_human Human No 8.4 EC50 = 4.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
461 7 2 6 4.8 CCCN(CCN1CCN(CC1)C2=C3C=CC=C(C3=NC=C2)O)C4CCC5=C(C4)C=CC=C5O
CHEMBL599636 drd2_human Human No 8.4 EC50 = 4.5 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
461 7 2 6 4.8 CCCN(CCN1CCN(CC1)C2=C3C=CC=C(C3=NC=C2)O)C4CCC5=C(C4)C=CC=C5O
CHEMBL419792 drd2_human Human Yes 8.3 EC50 = 4.6 Funct
Agonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counterAgonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counter
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL419792 drd2_human Human Yes 8.3 EC50 = 4.6 Funct
Agonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counterAgonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counter
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL135387 drd2_human Human No 8.3 EC50 = 4.9 Funct
In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptorIn vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor
393 6 1 4 4.0 C1CC(CCC1CCN2CCN(CC2)C3=CC=CC=N3)NC(=O)C4=CC=CC=C4
CHEMBL2397389 drd2_human Human No 6.4 EC50 = 400 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL2397389 drd2_human Human No 6.4 EC50 = 400 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
415 11 1 2 5.8 CCCN(CCCCNC(=O)C1=CC=C(C=C1)C2=CC=CC=C2)C3CCC(=CC3)C#C
CHEMBL269004 drd2_human Human Yes 7.4 EC50 = 41 Funct
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C=CC=C2O
CHEMBL556269 drd2_human Human No 7.4 EC50 = 41.2 Funct
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
461 7 2 4 4.3 CCCN(CCN1CCN(CC1)C(=O)C2=CC3=C(C=C2)NC=C3)C4CCC5=C(C4)C=CC=C5O
CHEMBL273273 drd2_human Human Yes 7.4 EC50 = 41.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C=CC=C2O
CHEMBL556269 drd2_human Human No 7.4 EC50 = 41.2 Funct
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
461 7 2 4 4.3 CCCN(CCN1CCN(CC1)C(=O)C2=CC3=C(C=C2)NC=C3)C4CCC5=C(C4)C=CC=C5O
CHEMBL273273 drd2_human Human Yes 7.4 EC50 = 41.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
247 5 1 2 4.1 CCCN(CCC)C1CCC2=C(C1)C=CC=C2O
CHEMBL3585367 drd2_human Human No 7.4 EC50 = 41.7 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
430 17 2 3 5.6 CCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3577343 drd2_human Human No 6.4 EC50 = 410 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3577343 drd2_human Human No 6.4 EC50 = 410 Funct
Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3798334 drd2_human Human No 5.4 EC50 = 4100 Funct
Agonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysisAgonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysis
420 8 1 5 4.7 COC1=CC=CC=C1N2CCN(CC2)CCCNC(=O)OC3=CC=CC4=CC=CC=C43
CHEMBL3798334 drd2_human Human No 5.4 EC50 = 4100 Funct
Agonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysisAgonist activity at human dopamine D2 receptor short isoform transfected in HEK293 cells measured for 10 mins by spectroscopic analysis
420 8 1 5 4.7 COC1=CC=CC=C1N2CCN(CC2)CCCNC(=O)OC3=CC=CC4=CC=CC=C43
CHEMBL3134066 drd2_human Human No 6.4 EC50 = 419 Funct
Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assayAgonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
787 17 4 8 7.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)OCCCNC(=O)CCCCCCC(=O)NCCCOC5=C(C6=C(CC7C8=C6C=CC=C8CCN7C)C=C5)O)O
CHEMBL3585367 drd2_human Human No 7.4 EC50 = 42 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
430 17 2 3 5.6 CCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL372020 drd2_rat Rat No 7.4 EC50 = 42 Funct
Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
245 5 0 2 3.0 CCCN(CCC)C1CCN2C(=CC=C2C#N)C1
CHEMBL3585367 drd2_human Human No 7.4 EC50 = 42 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
430 17 2 3 5.6 CCCCCCCCCC(=O)NCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL372020 drd2_rat Rat No 7.4 EC50 = 42 Funct
Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
245 5 0 2 3.0 CCCN(CCC)C1CCN2C(=CC=C2C#N)C1
CHEMBL85409 drd2_rat Rat No 6.4 EC50 = 427 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
277 3 3 4 2.6 C1CCC(C1)CC2CC3=C(C=CC(=C3O)O)C(O2)CN
CHEMBL557547 drd2_rat Rat No 7.4 EC50 = 43 Funct
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
281 0 2 3 2.7 CC1=CC2=C3C(CC4=C(C3=C1)C(=C(C=C4)O)O)N(CC2)C
CHEMBL557547 drd2_rat Rat No 7.4 EC50 = 43 Funct
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation countingAgonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
281 0 2 3 2.7 CC1=CC2=C3C(CC4=C(C3=C1)C(=C(C=C4)O)O)N(CC2)C
CHEMBL3800633 drd2_human Human No 7.4 EC50 = 43.3 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3800633 drd2_human Human No 7.4 EC50 = 43.3 Funct
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
418 7 2 4 3.3 CN(CCCCNC(=O)C1=CC2=CC=CC=C2O1)C3CC4=C5C(=CC=C4)NC(=O)N5C3
CHEMBL3287395 drd2_human Human No 6.4 EC50 = 436.5 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
491 10 0 6 5.2 CCOC(=O)C1=NN2C=CC(=CC2=C1)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL3613877 drd2_human Human No 5.4 EC50 = 4365.2 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
432 7 0 7 1.8 COC1=CC=CC=C1N2CCN(CC2)CCC3=CN(N=N3)C4=CC5=C(C=NN5C=C4)C=O
CHEMBL3613877 drd2_human Human No 5.4 EC50 = 4365.2 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay
432 7 0 7 1.8 COC1=CC=CC=C1N2CCN(CC2)CCC3=CN(N=N3)C4=CC5=C(C=NN5C=C4)C=O
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 44.7 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 44.7 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 44.7 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 44.7 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL1916549 drd2_human Human No 6.4 EC50 = 440 Funct
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
1122 39 2 12 12.1 CCCN(CCCCNC(=O)C1=CC(=C(C=C1)OCCCC2=CN(N=N2)CCCCCCCCN3C=C(N=N3)CCCOC4=C(C=C(C=C4)C(=O)NCCCCN(CCC)C5CC6=CC=CC=C6C5)OC)OC)C7CC8=CC=CC=C8C7
CHEMBL3287395 drd2_human Human No 6.4 EC50 = 440 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
491 10 0 6 5.2 CCOC(=O)C1=NN2C=CC(=CC2=C1)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL1916549 drd2_human Human No 6.4 EC50 = 440 Funct
Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assayAgonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay
1122 39 2 12 12.1 CCCN(CCCCNC(=O)C1=CC(=C(C=C1)OCCCC2=CN(N=N2)CCCCCCCCN3C=C(N=N3)CCCOC4=C(C=C(C=C4)C(=O)NCCCCN(CCC)C5CC6=CC=CC=C6C5)OC)OC)C7CC8=CC=CC=C8C7
CHEMBL3287395 drd2_human Human No 6.4 EC50 = 440 Funct
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
491 10 0 6 5.2 CCOC(=O)C1=NN2C=CC(=CC2=C1)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 45 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL155731 drd2_human Human Yes 7.4 EC50 = 45 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
246 2 1 4 1.9 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N
CHEMBL2165128 drd2_human Human No 4.3 EC50 = 46000 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
502 6 1 4 5.6 C1CC(CCC1CN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl)COC4=CC5=C(CCC(=O)N5)C=C4
CHEMBL3585373 drd2_human Human No 5.3 EC50 = 4677 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
375 12 3 5 -1.4 CCCN(CCCNC(=O)CCC(=O)O)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3585373 drd2_human Human No 5.3 EC50 = 4677 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
375 12 3 5 -1.4 CCCN(CCCNC(=O)CCC(=O)O)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL3585373 drd2_human Human No 5.3 EC50 = 4677.4 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
375 12 3 5 -1.4 CCCN(CCCNC(=O)CCC(=O)O)CCC1=C2CC(=O)NC2=CC=C1
CHEMBL310867 drd2_rat Rat Yes 7.3 EC50 = 47 Funct
Effective concentration required for agonistic activity against rat D2 short receptorEffective concentration required for agonistic activity against rat D2 short receptor
271 5 0 2 3.6 CCCN(CCC)C1CCC2=NN3C=CC=CC3=C2C1
CHEMBL3613878 drd2_human Human No 6.3 EC50 = 478.6 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
442 5 0 5 3.7 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3394253 drd2_human Human No 6.3 EC50 = 478.6 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
709 20 4 12 3.9 CCCN(CCCNC(=O)CCCC(=O)OC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL3613878 drd2_human Human No 6.3 EC50 = 478.6 Funct
Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assayActivity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay
442 5 0 5 3.7 C1CN(CCN1CCC2=CN(N=N2)C3=CC4=CC=NN4C=C3)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3394253 drd2_human Human No 6.3 EC50 = 478.6 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
709 20 4 12 3.9 CCCN(CCCNC(=O)CCCC(=O)OC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL3577343 drd2_human Human No 6.3 EC50 = 480 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3577343 drd2_human Human No 6.3 EC50 = 480 Funct
Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assayAgonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3394253 drd2_human Human No 6.3 EC50 = 484 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
709 20 4 12 3.9 CCCN(CCCNC(=O)CCCC(=O)OC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL449250 drd2_rat Rat Yes 7.3 EC50 = 49.5 Funct
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
274 3 1 3 1.7 CCCN1CCOC2C1CCC3=C2C=C(C=C3)C(=O)N
CHEMBL484599 drd2_rat Rat Yes 7.3 EC50 = 49.5 Funct
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 minAgonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
274 3 1 3 1.7 CCCN1CCOC2C1CCC3=C2C=C(C=C3)C(=O)N
CHEMBL160744 drd2_human Human No 8.3 EC50 = 5 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
408 7 1 4 4.1 CC1=C(C(=CC=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3)C
CHEMBL160921 drd2_human Human No 8.3 EC50 = 5 Funct
Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assayAgonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
405 7 1 5 3.1 C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC=C4C#N
CHEMBL3298828 drd2_human Human No 8.3 EC50 = 5.5 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
550 10 2 6 7.3 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCCN3CCC(CC3)C4=CC=C(C=C4)Cl)N
CHEMBL3298828 drd2_human Human No 8.3 EC50 = 5.5 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
550 10 2 6 7.3 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCCN3CCC(CC3)C4=CC=C(C=C4)Cl)N
CHEMBL3298828 drd2_human Human No 8.3 EC50 = 5.5 Funct
Partial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assayPartial agonist activity at human D2L receptor expressed in FlpIn CHO cells assessed as induction of ERK1/2 phosphorylation by AlphaScreen assay
550 10 2 6 7.3 CC1=C2C(=C(SC2=NC(=C1Cl)OC)C(=O)NCCCCCCN3CCC(CC3)C4=CC=C(C=C4)Cl)N
CHEMBL2165118 drd2_human Human No 8.3 EC50 = 5.6 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
448 6 1 4 4.8 C1CN(CCN(C1)C2=C(C(=CC=C2)Cl)Cl)CCCOC3=CC4=C(CCNC4=O)C=C3
CHEMBL2165134 drd2_human Human No 8.2 EC50 = 5.7 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
419 7 1 4 5.1 C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=NN3)C4=C(C(=CC=C4)Cl)Cl
CHEMBL2165132 drd2_human Human No 8.2 EC50 = 5.7 Funct
cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.cAMP GloSensor Assay: HEK293T cells co-expressing the cAMP biosensor GloSensor-22F (Promega) and hD2 receptors were seeded (10,000 cells/20 ul/well) into white, clear-bottom, tissue culture plates in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After a one- to two-hour recovery, cells were treated with 10 ul of 3x test or reference drug prepared in HBSS, 10% FBS, 20 mM HEPES, pH 7.4. After 30 minutes, cells were challenged with 10 ul of 1,200 nM (4x) isoproterenol in 8% (4x) GloSensor reagent. Luminescence per well per second was read on a Wallac TriLux microbeta plate counter. Data were normalized to the isoproterenol response (100%) and the maximal quinpirole-induced inhibition thereof (0%) and regressed using the sigmoidal dose-response function built into GraphPad Prism 4.0. Notably, HEK293T cells expressing the GloSensor-22F alone (no hD2) were assayed in parallel and displayed no inhibition of isoproterenol-stimulated cAMP.
482 5 1 4 5.3 C1CC(=O)NC2=C1C=CC(=C2)OC3=CC=C(C=C3)CN4CCN(CC4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL70565 drd2_rat Rat Yes 8.2 EC50 = 5.7 Funct
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat
249 2 1 4 2.0 CCCN1CCOC2C1COC3=C2C=C(C=C3)O
CHEMBL325710 drd2_rat Rat Yes 8.2 EC50 = 5.7 Funct
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity)
289 5 1 4 4.2 CCCN(CCC)C1CC2=CC3=C(C=C2C1)SC(=N3)N
CHEMBL53 drd2_human Human Yes 8.2 EC50 = 5.8 Funct
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_human Human Yes 8.2 EC50 = 5.8 Funct
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL53 drd2_human Human Yes 8.2 EC50 = 5.8 Funct
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
267 0 2 3 2.3 CN1CCC2=C3C1CC4=C(C3=CC=C2)C(=C(C=C4)O)O
CHEMBL2165138 drd2_human Human Yes 7.3 EC50 = 50 Funct
pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).pERK High-Content Assay: Cell Culture: Chinese Hamster Ovary (CHO) cells stably expressing the hD2L dopamine receptor (Urban et al., Neuropsychopharmacology 32:67 (2007)) were maintained in Ham's F12 medium supplemented with 10% fetal bovine serum, 100 U/mL penicillin, 100 ug/mL streptomycin, and 0.5 ug/ml G418. On day 1 of the assay, cells were seeded onto black clear-bottom tissue culture-treated 96-well plates (Greiner, BioOne). On day 2 of the assay, cells were washed with serum-free medium (Ham's F-12, penicillin and streptomycin) and incubated in 100 uL serum-free medium overnight.Immunofluorescence: Automatic multichannel pipetters were used for liquid handling and multichannel vacuum manifolds for aspirations. Each tested concentration was typically measured in triplicate or quadruplicate. For concentration curves, half-log-dilutions were used. Drug dilutions were prepared in stimulation medium (serum-free medium, 100 mg/L ascorbic acid).
421 6 0 4 6.2 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCOC3=CC4=C(C=C3)SC=N4
CHEMBL2165138 drd2_human Human Yes 7.3 EC50 = 50 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
421 6 0 4 6.2 C1CN(CCC1C2=C(C(=CC=C2)Cl)Cl)CCCOC3=CC4=C(C=C3)SC=N4
CHEMBL2165124 drd2_human Human No 7.3 EC50 = 50 Funct
Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayAgonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
424 9 1 5 3.7 CCOC1=CC=C(C=C1)N2CCN(CC2)CCCCOC3=CC4=C(CCC(=O)N4)C=C3
CHEMBL1079191 drd2_human Human No 7.3 EC50 = 50.1 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
322 4 0 2 2.9 C1CCCN(CC1)CCN2CCN(C2=O)C3=CC=C(C=C3)Cl
CHEMBL3394258 drd2_human Human No 6.3 EC50 = 501 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
822 27 5 12 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL2165132 drd2_human Human No 6.3 EC50 = 501 Funct
Partial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assayPartial agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay
482 5 1 4 5.3 C1CC(=O)NC2=C1C=CC(=C2)OC3=CC=C(C=C3)CN4CCN(CC4)C5=C(C(=CC=C5)Cl)Cl
CHEMBL3394258 drd2_human Human No 6.3 EC50 = 501.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
822 27 5 12 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL1077197 drd2_human Human No 6.3 EC50 = 501.2 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
260 3 1 3 0.5 C1CCNC(C1)CN2CCN(C2=O)C3=CN=CC=C3
CHEMBL3394258 drd2_human Human No 6.3 EC50 = 501.2 Funct
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
822 27 5 12 5.6 CCCN(CCCNC(=O)CCCCCCCNC(=O)CCCOC1=CC=C(C=C1)CCNC2=NC3=NC(=NN3C(=N2)N)C4=CC=CO4)CCC5=C6CC(=O)NC6=CC=C5
CHEMBL1077197 drd2_human Human No 6.3 EC50 = 501.2 Funct
Partial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assayPartial agonistic activity at human dopamine D2 receptor expressed in CHO cells by assay [35S]GTPgamma assay with scintillation proximity affinity assay
260 3 1 3 0.5 C1CCNC(C1)CN2CCN(C2=O)C3=CN=CC=C3
CHEMBL419792 drd2_human Human Yes 6.3 EC50 = 501.2 Funct
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assayAgonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
203 1 2 2 0.4 CNC1CC2=C3C(=CC=C2)NC(=O)N3C1
CHEMBL2114209 drd2_rat Rat No 5.3 EC50 = 5130 Funct
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary glandConcentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
223 2 3 4 1.0 CCC1CC2=C(C=CC(=C2O)O)C(O1)CN
CHEMBL3577342 drd2_human Human No 7.3 EC50 = 52 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL3577342 drd2_human Human No 7.3 EC50 = 52 Funct
Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assayIntrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay
552 19 1 7 5.0 CCCCN1C=C(N=N1)CCCOC2=C(C=C(C=C2)C(=O)NCCCCN(CCC)C3CC=C(OC3)C#C)OC
CHEMBL1254947 drd2_human Human No 7.3 EC50 = 52.6 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
470 8 1 4 6.5 CCCN(CCN1CCN(CC1)C2=CC=C(C=C2)C3=CC=CC=C3)C4CCC5=C(C4)C=CC=C5O
CHEMBL1254947 drd2_human Human No 7.3 EC50 = 52.6 Funct
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding