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
CHEMBL236039 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
504 11 6 6 3.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL230486 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
463 11 5 5 3.2 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1242943 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
576 12 6 8 2.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=C(C=C(C=C2)O)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL236039 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
504 11 6 6 3.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL230486 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
463 11 5 5 3.2 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1242943 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
576 12 6 8 2.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=C(C=C(C=C2)O)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL236041 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
488 10 5 5 3.8 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)N(C)CC3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL236041 adrb2_human Human No 10.7 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
488 10 5 5 3.8 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)N(C)CC3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1243189 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
526 12 5 7 2.5 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243189 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
526 12 5 7 2.5 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL230490 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
517 11 5 5 4.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL230490 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
517 11 5 5 4.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1243158 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
512 12 5 7 2.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243158 adrb2_human Human No 10.6 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
512 12 5 7 2.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL430361 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
481 10 6 7 2.6 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=NC=CS3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL430361 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
481 10 6 7 2.6 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=NC=CS3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1221680 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
400 7 4 6 2.4 C1CC(C(C1)OCC2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1221680 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
400 7 4 6 2.4 C1CC(C(C1)OCC2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1243348 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
518 12 5 7 3.2 CC(CC1=CC=CC(=C1)CC(=O)NCC2CCCCC2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243348 adrb2_human Human No 10.5 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
518 12 5 7 3.2 CC(CC1=CC=CC(=C1)CC(=O)NCC2CCCCC2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL236040 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
520 11 6 6 4.1 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3SC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL391006 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
475 10 6 6 2.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=N3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL236040 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
520 11 6 6 4.1 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3SC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL391006 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
475 10 6 6 2.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=N3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1243256 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
542 13 5 8 2.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2OC)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243190 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
526 13 5 7 2.8 CC(CC1=CC=CC(=C1)CC(=O)NCCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243256 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
542 13 5 8 2.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2OC)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243190 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
526 13 5 7 2.8 CC(CC1=CC=CC(=C1)CC(=O)NCCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243222 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
540 14 5 7 3.2 CC(CC1=CC=CC(=C1)CC(=O)NCCCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243222 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
540 14 5 7 3.2 CC(CC1=CC=CC(=C1)CC(=O)NCCCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243101 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
570 12 6 8 2.9 CC1=CC(=CC(=C1CNC(=O)CC2=CC(=CC=C2)CC(C)(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O)C)O
CHEMBL1243101 adrb2_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
570 12 6 8 2.9 CC1=CC(=CC(=C1CNC(=O)CC2=CC(=CC=C2)CC(C)(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O)C)O
CHEMBL1243285 adrb2_human Human No 10.3 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
556 14 5 8 2.7 CCOC1=CC=CC=C1CNC(=O)CC2=CC(=CC=C2)CC(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243285 adrb2_human Human No 10.3 EC50 = 0.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
556 14 5 8 2.7 CCOC1=CC=CC=C1CNC(=O)CC2=CC(=CC=C2)CC(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL391946 adrb2_human Human No 10.3 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
474 10 6 5 3.6 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL391946 adrb2_human Human No 10.3 EC50 = 0.0 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
474 10 6 5 3.6 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1682213 adrb2_cavpo Guinea pig No 10.3 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
501 11 6 5 3.0 C1=CC=C(C=C1)CCCNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682213 adrb2_cavpo Guinea pig No 10.3 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
501 11 6 5 3.0 C1=CC=C(C=C1)CCCNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1940832 adrb2_cavpo Guinea pig Yes 10.3 EC50 = 0.1 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1940832 adrb2_cavpo Guinea pig Yes 10.3 EC50 = 0.1 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL236251 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
452 10 6 5 3.4 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3CCC3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL236251 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
452 10 6 5 3.4 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3CCC3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL235612 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
510 10 6 7 3.8 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3F)F)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL235612 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
510 10 6 7 3.8 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3F)F)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1243407 adrb2_human Human Yes 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
378 8 4 6 1.8 CC(C)(CC1=CC=CC=C1)NCC(C2=CC(=C(C=C2)O)NS(=O)(=O)C)O
CHEMBL1243407 adrb2_human Human Yes 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
378 8 4 6 1.8 CC(C)(CC1=CC=CC=C1)NCC(C2=CC(=C(C=C2)O)NS(=O)(=O)C)O
CHEMBL1243317 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
540 12 5 7 3.1 CC1=C(C=C(C=C1)CNC(=O)CC2=CC(=CC=C2)CC(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O)C
CHEMBL1243317 adrb2_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
540 12 5 7 3.1 CC1=C(C=C(C=C1)CNC(=O)CC2=CC(=CC=C2)CC(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O)C
CHEMBL392056 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
488 10 6 5 4.0 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NC(C)C3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL237501 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
534 12 6 7 3.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL392056 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
488 10 6 5 4.0 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NC(C)C3=CC=CC=C3)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL237501 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
534 12 6 7 3.5 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1807817 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
449 13 4 7 2.9 C1=CC=C(C=C1)CCOCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL3298987 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
579 12 6 7 4.5 CC(C)(COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5)N
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1807817 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
449 13 4 7 2.9 C1=CC=C(C=C1)CCOCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL3298987 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
579 12 6 7 4.5 CC(C)(COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5)N
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1940832 adrb2_human Human Yes 10.2 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL402501 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
493 10 5 5 4.2 CC(CC1=CC=CC(=C1)CC(=O)NC23CC4CC(C2)CC(C4)C3)NCC(C5=CC(=C(C=C5)O)CO)O
CHEMBL402501 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
493 10 5 5 4.2 CC(CC1=CC=CC(=C1)CC(=O)NC23CC4CC(C2)CC(C4)C3)NCC(C5=CC(=C(C=C5)O)CO)O
CHEMBL1243347 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
595 12 5 7 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243347 adrb2_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
595 12 5 7 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1682210 adrb2_cavpo Guinea pig No 10.2 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
459 8 6 5 2.2 C1=CC=C(C=C1)NC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682210 adrb2_cavpo Guinea pig No 10.2 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
459 8 6 5 2.2 C1=CC=C(C=C1)NC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1807818 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
449 13 4 7 2.9 C1=CC=C(C=C1)CCOCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807819 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
463 14 4 7 3.2 C1=CC=C(C=C1)CCOCCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3298986 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
503 11 6 7 2.8 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N
CHEMBL3298325 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC(=CC=C5)CN
CHEMBL1807818 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
449 13 4 7 2.9 C1=CC=C(C=C1)CCOCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807819 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
463 14 4 7 3.2 C1=CC=C(C=C1)CCOCCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3298986 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
503 11 6 7 2.8 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N
CHEMBL3298325 adrb2_human Human No 10.1 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC(=CC=C5)CN
CHEMBL1682212 adrb2_cavpo Guinea pig No 10.1 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
487 10 6 5 2.6 C1=CC=C(C=C1)CCNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682212 adrb2_cavpo Guinea pig No 10.1 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
487 10 6 5 2.6 C1=CC=C(C=C1)CCNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1243068 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
611 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C(=C2)Cl)O)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243068 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
611 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C(=C2)Cl)O)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL230203 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
435 11 5 5 2.6 C1=CC=C(C=C1)CNC(=O)CC2=CC(=CC=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL230487 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
449 11 5 5 3.0 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL230203 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
435 11 5 5 2.6 C1=CC=C(C=C1)CNC(=O)CC2=CC(=CC=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL230487 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
449 11 5 5 3.0 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC=C2)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1951067 adrb2_cavpo Guinea pig No 10.0 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
539 12 4 8 2.7 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCNCC(C4=CC(=C(C=C4)O)NC=O)O)OC
CHEMBL568272 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
372 6 5 6 1.5 CC(C)(CC1=CC=C(C=C1)O)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL579394 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
370 6 4 5 2.2 CC1=CC=CC=C1CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1807820 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
499 13 4 7 4.1 C1=CC=C2C(=C1)C=CC=C2CCOCCSCCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3426706 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 14 6 8 4.3 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC=CC(=C4)CCNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298326 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=C(C=C5)CN
CHEMBL3298328 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
475 11 6 7 2.2 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCN
CHEMBL1940830 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1951067 adrb2_cavpo Guinea pig No 10.0 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
539 12 4 8 2.7 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCNCC(C4=CC(=C(C=C4)O)NC=O)O)OC
CHEMBL568272 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
372 6 5 6 1.5 CC(C)(CC1=CC=C(C=C1)O)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL579394 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
370 6 4 5 2.2 CC1=CC=CC=C1CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1807820 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
499 13 4 7 4.1 C1=CC=C2C(=C1)C=CC=C2CCOCCSCCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3426706 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 14 6 8 4.3 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC=CC(=C4)CCNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298326 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=C(C=C5)CN
CHEMBL3298328 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
475 11 6 7 2.2 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCN
CHEMBL1940830 adrb2_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL235818 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
553 11 7 8 2.1 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=C(C=C3)S(=O)(=O)N)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL235818 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
553 11 7 8 2.1 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=C(C=C3)S(=O)(=O)N)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1807821 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
433 13 4 7 2.1 C1=CC=C(C=C1)CCOCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807822 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
483 13 4 7 3.3 C1=CC=C2C(=C1)C=CC=C2CCOCCOCCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3426697 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
656 16 6 8 3.5 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3290999 adrb2_human Human Yes 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3298330 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
503 13 6 7 2.9 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCCN
CHEMBL3298324 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5CN
CHEMBL3298897 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
544 12 6 8 2.5 C1CN(CCN1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3290999 adrb2_human Human Yes 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3290998 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
498 11 5 6 4.6 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)C4=CC=CC=C4
CHEMBL1940833 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 6 6 2.5 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)O
CHEMBL1363 adrb2_cavpo Guinea pig Yes 9.9 EC50 = 0.1 Funct
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1807821 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
433 13 4 7 2.1 C1=CC=C(C=C1)CCOCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807822 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
483 13 4 7 3.3 C1=CC=C2C(=C1)C=CC=C2CCOCCOCCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3426697 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
656 16 6 8 3.5 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3290999 adrb2_human Human Yes 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3298330 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
503 13 6 7 2.9 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCCN
CHEMBL3298324 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5CN
CHEMBL3298897 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
544 12 6 8 2.5 C1CN(CCN1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3290999 adrb2_human Human Yes 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3290998 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
498 11 5 6 4.6 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)C4=CC=CC=C4
CHEMBL1940833 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 6 6 2.5 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)O
CHEMBL1682214 adrb2_cavpo Guinea pig No 9.9 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
516 10 7 6 1.0 C1=CC(=CC(=C1)NC(=O)NCC2=CC=CC(=C2)C(=O)N)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1243035 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
611 12 6 8 4.0 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=CC(=C2O)Cl)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1682214 adrb2_cavpo Guinea pig No 9.9 EC50 = 0.1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
516 10 7 6 1.0 C1=CC(=CC(=C1)NC(=O)NCC2=CC=CC(=C2)C(=O)N)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1243035 adrb2_human Human No 9.9 EC50 = 0.1 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
611 12 6 8 4.0 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=CC(=C2O)Cl)Cl)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL3426701 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
704 13 6 8 4.7 CC1=CC(=C(C=C1C(=O)NCCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)C)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426698 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
682 13 6 8 4.0 C1CC(CCC1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3298691 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
519 14 6 8 2.1 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCOCCN
CHEMBL3298329 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
489 12 6 7 2.6 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCN
CHEMBL1944691 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL3426701 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
704 13 6 8 4.7 CC1=CC(=C(C=C1C(=O)NCCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)C)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426698 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
682 13 6 8 4.0 C1CC(CCC1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3298691 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
519 14 6 8 2.1 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCOCCN
CHEMBL3298329 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
489 12 6 7 2.6 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCN
CHEMBL1944691 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL394339 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
490 10 7 6 3.2 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL394339 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
490 10 7 6 3.2 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1243000 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
576 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=C(C=CC(=C2)Cl)O)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1243000 adrb2_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
576 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=C(C=CC(=C2)Cl)O)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945032 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=C(C=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1800472 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
460 12 4 7 1.3 CN(CCNCC(C1=C2C(=C(C=C1)O)NC(=O)S2)O)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807872 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
466 13 5 7 2.4 C1=CC(=CC(=C1)Cl)CCNCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3426693 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 6 8 4.2 CC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426694 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 6 8 4.2 CC1=C(C=CC(=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945034 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1682216 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
491 9 6 6 2.3 C1=CC(=CC(=C1)NC(=O)NCC2=CC=C(C=C2)F)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682215 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
503 10 6 6 2.1 COC1=CC=CC=C1CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682218 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
549 10 6 5 3.8 C1=CC=C(C=C1)C(C2=CC=CC=C2)NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1682217 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
541 9 6 5 3.4 C1=CC(=CC(=C1)NC(=O)NCC2=C(C=CC=C2Cl)Cl)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682211 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
473 9 6 5 2.2 C1=CC=C(C=C1)CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL567863 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
356 6 4 5 1.8 CC(C)(CC1=CC=CC=C1)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1945032 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=C(C=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1682216 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
491 9 6 6 2.3 C1=CC(=CC(=C1)NC(=O)NCC2=CC=C(C=C2)F)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682215 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
503 10 6 6 2.1 COC1=CC=CC=C1CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682218 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
549 10 6 5 3.8 C1=CC=C(C=C1)C(C2=CC=CC=C2)NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1682217 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
541 9 6 5 3.4 C1=CC(=CC(=C1)NC(=O)NCC2=C(C=CC=C2Cl)Cl)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1682211 adrb2_cavpo Guinea pig No 9.7 EC50 = 0.2 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
473 9 6 5 2.2 C1=CC=C(C=C1)CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL567863 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
356 6 4 5 1.8 CC(C)(CC1=CC=CC=C1)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1800472 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
460 12 4 7 1.3 CN(CCNCC(C1=C2C(=C(C=C1)O)NC(=O)S2)O)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807872 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
466 13 5 7 2.4 C1=CC(=CC(=C1)Cl)CCNCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3426693 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 6 8 4.2 CC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426694 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 6 8 4.2 CC1=C(C=CC(=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945034 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1256786 adrb2_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1240965 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
592 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC3=C(C=C2)C=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL1240965 adrb2_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
592 12 6 8 3.4 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC3=C(C=C2)C=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL1240966 adrb2_human Human No 9.6 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
618 13 6 8 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=C(C=C2)C3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL1240966 adrb2_human Human No 9.6 EC50 = 0.2 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
618 13 6 8 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=C(C=C2)C3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL1221681 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
400 7 4 6 2.4 C1CC(C(C1)OCC2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1221681 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
400 7 4 6 2.4 C1CC(C(C1)OCC2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947151 adrb2_cavpo Guinea pig No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
524 11 4 5 6.0 CC(C1=CC=CC=C1)NCC2=CC=CC=C2C3=CC=C(C=C3)CCNCCC4=C5C(=C(C=C4)O)NC(=O)S5
CHEMBL1944691 adrb2_cavpo Guinea pig No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL3426691 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.8 COC1=C(C=CC(=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426695 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 14 6 9 4.1 CC1=C(C=CC(=C1OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426702 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 5 8 4.1 CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426688 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
710 13 6 8 4.4 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=C(C=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O)Cl
CHEMBL3039518 adrb2_human Human Yes 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
740 14 6 9 4.4 COC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426687 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
676 13 6 8 3.8 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298213 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
479 12 6 7 2.6 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)N
CHEMBL3298327 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
460 10 5 6 3.5 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1944695 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
464 11 5 6 3.3 C1=CC=C(C=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1944690 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
498 11 5 6 4.0 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1945032 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=C(C=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1947151 adrb2_cavpo Guinea pig No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
524 11 4 5 6.0 CC(C1=CC=CC=C1)NCC2=CC=CC=C2C3=CC=C(C=C3)CCNCCC4=C5C(=C(C=C4)O)NC(=O)S5
CHEMBL1944691 adrb2_cavpo Guinea pig No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL3426691 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.8 COC1=C(C=CC(=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426695 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 14 6 9 4.1 CC1=C(C=CC(=C1OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426702 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
690 13 5 8 4.1 CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426688 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
710 13 6 8 4.4 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=C(C=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O)Cl
CHEMBL3039518 adrb2_human Human Yes 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
740 14 6 9 4.4 COC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426687 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
676 13 6 8 3.8 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298213 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
479 12 6 7 2.6 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)N
CHEMBL3298327 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
460 10 5 6 3.5 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1944695 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
464 11 5 6 3.3 C1=CC=C(C=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1944690 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
498 11 5 6 4.0 C1=CC=C(C(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1945032 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=C(C=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL236042 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
518 12 6 6 4.0 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCCC3=CC(=CC=C3)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL236042 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
518 12 6 6 4.0 CC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCCC3=CC(=CC=C3)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL391308 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
548 13 6 7 4.0 CCC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL391308 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
548 13 6 7 4.0 CCC(CC1=CC2=C(C=C1)NC(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1240967 adrb2_human Human Yes 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
618 13 6 8 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC(=C2)C3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL1240967 adrb2_human Human Yes 9.6 EC50 = 0.3 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
618 13 6 8 3.8 CC(C)(CC1=CC=CC(=C1)CC(=O)NCC2=CC=CC(=C2)C3=CC=C(C=C3)O)NCC(C4=CC(=C(C=C4)O)NS(=O)(=O)C)O
CHEMBL2088201 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
407 6 4 4 3.5 CCC1=C(C=C2CC(CC2=C1)(C)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
CHEMBL2088201 adrb2_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
407 6 4 4 3.5 CCC1=C(C=C2CC(CC2=C1)(C)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
CHEMBL228992 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
317 7 4 5 2.3 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL388570 adrb2_human Human Yes 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
303 6 5 5 2.0 CC(CC1=CC=C(C=C1)O)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL228992 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
317 7 4 5 2.3 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL388570 adrb2_human Human Yes 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
303 6 5 5 2.0 CC(CC1=CC=C(C=C1)O)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL228992 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
317 7 4 5 2.3 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL1363 adrb2_cavpo Guinea pig Yes 9.5 EC50 = 0.3 Funct
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945033 adrb2_cavpo Guinea pig No 9.5 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1363 adrb2_human Human Yes 9.5 EC50 = 0.3 Funct
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL3426696 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 14 6 9 4.1 CC1=CC(=C(C=C1NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)OC)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298831 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
545 12 5 8 2.8 C1COCCN1CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298325 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC(=CC=C5)CN
CHEMBL1944689 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
532 11 5 6 4.6 C1=CC(=C(C(=C1)Cl)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1944694 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1944693 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945031 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=CC(=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1945041 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
484 10 5 6 3.5 C1=CC=C(C(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1940831 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940815 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940817 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
451 11 6 6 3.4 CC(C)(CC1=CC=C(C=C1)NCC(C2=CC=CC=C2)O)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1256786 adrb2_cavpo Guinea pig Yes 9.5 EC50 = 0.3 Funct
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945033 adrb2_cavpo Guinea pig No 9.5 EC50 = 0.3 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3426696 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 14 6 9 4.1 CC1=CC(=C(C=C1NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)OC)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298831 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
545 12 5 8 2.8 C1COCCN1CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298325 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC(=CC=C5)CN
CHEMBL1944689 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
532 11 5 6 4.6 C1=CC(=C(C(=C1)Cl)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1944694 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1944693 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945031 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
517 11 6 6 3.8 CC1=CC=CC2=C1NC=C2CCNCC3=CC=CC(=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1945041 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
484 10 5 6 3.5 C1=CC=C(C(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)Cl
CHEMBL1940831 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940815 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940817 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
451 11 6 6 3.4 CC(C)(CC1=CC=C(C=C1)NCC(C2=CC=CC=C2)O)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1683933 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
627 16 5 7 5.7 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1683933 adrb2_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
627 16 5 7 5.7 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1683934 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1683934 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1242969 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
604 13 5 8 3.4 CCN(CC1=C(C=C(C=C1)O)Cl)C(=O)CC2=CC(=CC=C2)CC(C)(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1242969 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
604 13 5 8 3.4 CCN(CC1=C(C=C(C=C1)O)Cl)C(=O)CC2=CC(=CC=C2)CC(C)(C)NCC(C3=CC(=C(C=C3)O)NS(=O)(=O)C)O
CHEMBL1807870 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC=C(C(=C1)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)Cl
CHEMBL1683934 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3426692 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
740 14 6 9 4.4 COC1=C(C=CC(=C1Cl)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3290999 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL1945299 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CNCCC2=CC(=CC=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945036 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
478 11 5 6 3.7 CC(CNCC1=CC=C(C=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)C4=CC=CC=C4
CHEMBL1944692 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL3290999 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL1940816 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
424 11 5 6 2.7 C1=CC=C(C=C1)C(COC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940834 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 5 5 4.0 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C(=C3)Cl)N)Cl)O)O
CHEMBL1807870 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC=C(C(=C1)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)Cl
CHEMBL1683934 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3426692 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
740 14 6 9 4.4 COC1=C(C=CC(=C1Cl)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3290999 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL1945299 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
494 12 5 7 3.3 COC1=CC=CC=C1CNCCC2=CC(=CC=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945036 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
478 11 5 6 3.7 CC(CNCC1=CC=C(C=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)C4=CC=CC=C4
CHEMBL1944692 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC2=CC=C(C=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL3290999 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL1940816 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
424 11 5 6 2.7 C1=CC=C(C=C1)C(COC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940834 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 5 5 4.0 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C(=C3)Cl)N)Cl)O)O
CHEMBL1256786 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL584498 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC=C(C=C1)C(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL567833 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
370 6 4 5 2.2 CC1=CC(=CC=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1800961 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
337 6 4 4 3.9 CC(CC1=CC2=CC=CC=C2C=C1)NCC(C3=CC(=CC(=C3)O)O)O
CHEMBL1256786 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1363 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL584498 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC=C(C=C1)C(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL567833 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
370 6 4 5 2.2 CC1=CC(=CC=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1800961 adrb2_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
337 6 4 4 3.9 CC(CC1=CC2=CC=CC=C2C=C1)NCC(C3=CC(=CC(=C3)O)O)O
CHEMBL1363 adrb2_human Human Yes 9.4 EC50 = 0.4 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL565267 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
392 6 4 7 2.0 CC(C)(CC1=CC(=CC(=C1)F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL576428 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
542 13 6 8 0.7 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN(C)C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL565267 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
392 6 4 7 2.0 CC(C)(CC1=CC(=CC(=C1)F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL576428 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
542 13 6 8 0.7 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN(C)C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1951066 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
539 12 4 8 2.7 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCNCC(C4=CC(=C(C=C4)O)NC=O)O)OC
CHEMBL1945039 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947152 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
510 11 4 5 5.6 C1=CC=C(C=C1)CNCC2=CC=CC(=C2)C3=CC(=CC=C3)CCNCCC4=C5C(=C(C=C4)O)NC(=O)S5
CHEMBL1940832 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1363 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1256786 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL323776 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
444 12 3 6 2.4 CN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807832 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
466 13 5 7 2.4 C1=CC(=CC(=C1)Cl)CCNCCCOCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3426699 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
676 13 6 8 4.0 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCNC(=O)C4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426689 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.8 COC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426690 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
710 13 6 8 4.4 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC(=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O)Cl
CHEMBL3298692 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
575 14 6 8 3.9 CC(C)(C)OC(=O)NCCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL3298762 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
579 13 6 7 4.1 C1=CC=C(C=C1)C(=O)NCCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1940832 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL3298326 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=C(C=C5)CN
CHEMBL3298328 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
475 11 6 7 2.2 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCN
CHEMBL1947157 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
532 11 5 6 4.6 C1=CC(=CC(=C1)CNCCC2=C(C=CC=C2Cl)Cl)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945033 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945037 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
478 12 5 6 3.7 C1=CC=C(C=C1)CCCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1256786 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL3290997 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL1951066 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
539 12 4 8 2.7 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCNCC(C4=CC(=C(C=C4)O)NC=O)O)OC
CHEMBL1945039 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947152 adrb2_cavpo Guinea pig No 9.3 EC50 = 0.5 Funct
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
510 11 4 5 5.6 C1=CC=C(C=C1)CNCC2=CC=CC(=C2)C3=CC(=CC=C3)CCNCCC4=C5C(=C(C=C4)O)NC(=O)S5
CHEMBL1940832 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL1256786 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1256786 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL323776 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
444 12 3 6 2.4 CN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807832 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
466 13 5 7 2.4 C1=CC(=CC(=C1)Cl)CCNCCCOCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3426699 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
676 13 6 8 4.0 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCNC(=O)C4=CC=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426689 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.8 COC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426690 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
710 13 6 8 4.4 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCC(=O)NC4=CC(=C(C=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O)Cl
CHEMBL3298692 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
575 14 6 8 3.9 CC(C)(C)OC(=O)NCCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL3298762 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
579 13 6 7 4.1 C1=CC=C(C=C1)C(=O)NCCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1940832 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
436 11 6 6 2.3 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)O
CHEMBL3298326 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=C(C=C5)CN
CHEMBL3298328 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
475 11 6 7 2.2 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCN
CHEMBL1947157 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
532 11 5 6 4.6 C1=CC(=CC(=C1)CNCCC2=C(C=CC=C2Cl)Cl)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945033 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 11 5 7 2.3 C1=CC=NC(=C1)CCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945037 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
478 12 5 6 3.7 C1=CC=C(C=C1)CCCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1256786 adrb2_human Human Yes 9.3 EC50 = 0.5 Funct
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL3290997 adrb2_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL567192 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
384 7 4 5 2.6 CCC1=CC=C(C=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL568273 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC(=CC=C1)C(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL567192 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
384 7 4 5 2.6 CCC1=CC=C(C=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL568273 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC(=CC=C1)C(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL2335415 adrb2_cavpo Guinea pig No 9.2 EC50 = 0.6 Funct
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
554 14 4 8 3.8 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCCCNCC(C4=CC(=C(C=C4)O)CO)O)OC
CHEMBL1807828 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC=C(C(=C1)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)Cl
CHEMBL1807831 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
514 13 5 8 1.9 C1=CC(=CC(=C1)Cl)CCNCCCS(=O)(=O)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL82663 adrb2_human Human Yes 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL1807828 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC=C(C(=C1)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)Cl
CHEMBL1807831 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
514 13 5 8 1.9 C1=CC(=CC(=C1)Cl)CCNCCCS(=O)(=O)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL82663 adrb2_human Human Yes 9.2 EC50 = 0.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL3298832 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
622 13 5 10 2.3 CS(=O)(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298832 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
622 13 5 10 2.3 CS(=O)(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298330 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
503 13 6 7 2.9 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCCN
CHEMBL3298987 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
579 12 6 7 4.5 CC(C)(COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5)N
CHEMBL3298691 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
519 14 6 8 2.1 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCOCCN
CHEMBL3298329 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
489 12 6 7 2.6 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCN
CHEMBL3298330 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
503 13 6 7 2.9 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCCN
CHEMBL3298987 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
579 12 6 7 4.5 CC(C)(COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5)N
CHEMBL3298691 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
519 14 6 8 2.1 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCOCCN
CHEMBL3298329 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
489 12 6 7 2.6 C1=CC(=CC=C1CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC4=CC=C(C=C4)OCCCN
CHEMBL1945042 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
468 10 5 7 3.0 C1=CC=C(C(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL1945039 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945043 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
451 10 5 7 1.8 C1=CC=NC(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945294 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
414 8 4 6 2.3 C1CCN(C1)CC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947156 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
526 11 5 6 4.5 C1=CC=C(C=C1)CNCC2=CC=CC(=C2)C3=CC(=CC=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL82663 adrb2_human Human Yes 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL1945042 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
468 10 5 7 3.0 C1=CC=C(C(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O)F
CHEMBL1945039 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=CC=C1CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945043 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
451 10 5 7 1.8 C1=CC=NC(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945294 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
414 8 4 6 2.3 C1CCN(C1)CC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947156 adrb2_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
526 11 5 6 4.5 C1=CC=C(C=C1)CNCC2=CC=CC(=C2)C3=CC(=CC=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL82663 adrb2_human Human Yes 9.2 EC50 = 0.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
465 13 3 7 2.7 C1=CC=C(C=C1)CCOCCCS(=O)(=O)CCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL2335412 adrb2_cavpo Guinea pig No 9.2 EC50 = 0.6 Funct
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
498 10 4 8 2.4 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCNCC(C4=CC(=C(C=C4)O)CO)O)OC
CHEMBL2335413 adrb2_cavpo Guinea pig No 9.2 EC50 = 0.7 Funct
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
526 12 4 8 3.1 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCNCC(C4=CC(=C(C=C4)O)CO)O)OC
CHEMBL238347 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
624 14 5 7 5.1 CC(CC1=CC2=C(C=C1)N(C(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)CC4=CC=CC=C4)NCC(C5=CC(=C(C=C5)O)CO)O
CHEMBL238347 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
624 14 5 7 5.1 CC(CC1=CC2=C(C=C1)N(C(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)CC4=CC=CC=C4)NCC(C5=CC(=C(C=C5)O)CO)O
CHEMBL1682219 adrb2_cavpo Guinea pig No 9.2 EC50 = 0.7 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
535 9 6 5 3.8 C1=CC=C(C=C1)C2=CC=CC=C2NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL568531 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
440 7 4 9 3.0 CC(C)(CC1=CC=C(C=C1)OC(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL601036 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
370 6 4 5 2.2 CC1=CC=CC=C1CC(C)(C)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL1682219 adrb2_cavpo Guinea pig No 9.2 EC50 = 0.7 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
535 9 6 5 3.8 C1=CC=C(C=C1)C2=CC=CC=C2NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL568531 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
440 7 4 9 3.0 CC(C)(CC1=CC=C(C=C1)OC(F)(F)F)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL601036 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
370 6 4 5 2.2 CC1=CC=CC=C1CC(C)(C)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL428027 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
548 12 5 7 3.5 CC(CC1=CC2=C(C=C1)N(C(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)C)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL428027 adrb2_human Human No 9.2 EC50 = 0.7 Funct
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
548 12 5 7 3.5 CC(CC1=CC2=C(C=C1)N(C(=C2)C(=O)NCC3=C(C=CC=C3OC)OC)C)NCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1814277 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
526 17 5 7 2.7 C1=CC(=CC(=C1)N2C(=O)C=CNC2=O)CCCCOCCCCCCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1800660 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
502 15 4 7 2.5 CCCCN(CCNCC(C1=C2C(=C(C=C1)O)NC(=O)S2)O)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807823 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
448 13 5 7 2.6 C1=CC=C(C=C1)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807873 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
500 13 5 7 3.0 C1=CC(=C(C(=C1)Cl)Cl)CCNCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1346 adrb2_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL3426703 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
754 14 5 9 4.6 CN(C1=C(C=C(C(=C1)OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426708 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 15 6 9 4.2 COC1=C(C=C(C=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CCNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298324 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5CN
CHEMBL1945297 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
547 11 5 6 5.0 CC(CC1=CC(=CC=C1)CNCCC2=C(C=CC=C2Cl)Cl)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945289 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=C(C=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3290998 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
498 11 5 6 4.6 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)C4=CC=CC=C4
CHEMBL1814277 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
526 17 5 7 2.7 C1=CC(=CC(=C1)N2C(=O)C=CNC2=O)CCCCOCCCCCCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1800660 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
502 15 4 7 2.5 CCCCN(CCNCC(C1=C2C(=C(C=C1)O)NC(=O)S2)O)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807823 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
448 13 5 7 2.6 C1=CC=C(C=C1)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807873 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
500 13 5 7 3.0 C1=CC(=C(C(=C1)Cl)Cl)CCNCCOCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1346 adrb2_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL3426703 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
754 14 5 9 4.6 CN(C1=C(C=C(C(=C1)OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426708 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 15 6 9 4.2 COC1=C(C=C(C=C1)NC(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CCNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298324 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
551 11 6 7 3.7 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5CN
CHEMBL1945297 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
547 11 5 6 5.0 CC(CC1=CC(=CC=C1)CNCCC2=C(C=CC=C2Cl)Cl)NCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945289 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=C(C=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3290998 adrb2_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
498 11 5 6 4.6 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)NC=O)O)C4=CC=CC=C4
CHEMBL1346 adrb2_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL1346 adrb2_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL2335414 adrb2_cavpo Guinea pig No 9.1 EC50 = 0.8 Funct
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
540 13 4 8 3.5 COC1=C(C=C(C=C1)C2=NN(C(=O)C3C2CCCC3)CCCCCNCC(C4=CC(=C(C=C4)O)CO)O)OC
CHEMBL1682302 adrb2_cavpo Guinea pig No 9.1 EC50 = 0.9 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
529 10 6 5 3.8 CC(C)(C)C1=CC=C(C=C1)CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL568239 adrb2_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
528 13 7 8 -0.4 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CCN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1683942 adrb2_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
723 18 5 10 4.9 C[N+]1(C2CC(CC1C3C2O3)OC(=O)C(C4=CC=CS4)(C5=CC=CS5)O)CCCCCCCCCNCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL1682302 adrb2_cavpo Guinea pig No 9.1 EC50 = 0.9 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
529 10 6 5 3.8 CC(C)(C)C1=CC=C(C=C1)CNC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL568239 adrb2_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
528 13 7 8 -0.4 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CCN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1683942 adrb2_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
723 18 5 10 4.9 C[N+]1(C2CC(CC1C3C2O3)OC(=O)C(C4=CC=CS4)(C5=CC=CS5)O)CCCCCCCCCNCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL1346 adrb2_cavpo Guinea pig Yes 9.0 EC50 = 1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL1682221 adrb2_cavpo Guinea pig No 9.0 EC50 = 1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
551 10 6 6 3.7 C1=CC=C(C=C1)OC2=CC=CC(=C2)NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1814279 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
532 19 7 8 0.2 C1=CC(=CC(=C1)NC(=O)NCC(=O)O)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O
CHEMBL1800656 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
458 13 3 6 2.8 CCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807827 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC(=CC(=C1)Cl)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1256786 adrb2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL3298986 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
503 11 6 7 2.8 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N
CHEMBL577917 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
499 11 7 7 -0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCN=C(N)N)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1256786 adrb2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945038 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
479 12 5 7 2.6 C1=CC=NC(=C1)CCCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947153 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
504 9 4 6 4.1 C1CN(CCC1C2=CC=CC=C2)CC3=CC=CC(=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1945044 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=CC(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3645329 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 18 6 9 5.1 CN(C1=CC=C(C=C1)CC(=O)NCC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645278 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
839 18 6 10 4.2 CN(CCCC(=O)NC1=C(C=C(C(=C1)OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645288 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
803 19 6 9 4.4 CN(CCCCC(=O)NC1=CC=C(C=C1)CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645354 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 5.9 CC(CC1=CC=CC(=C1)CCC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645335 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 18 6 9 5.9 CC1=C(C=CC=C1CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)CC(C)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645299 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.6 CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645341 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645304 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC(=CC=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645313 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC=C(C=C1)CNC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3666068 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
817 18 6 9 4.7 CC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C)NC(=O)CCCCN(C)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645363 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
789 18 6 9 3.9 CN(CCCCC(=O)NC1=CC=C(C=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645303 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC(=CC=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645286 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
853 19 6 10 4.5 CN(CCCCC(=O)NC1=C(C=C(C(=C1)OC)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645296 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 15 6 9 5.5 CC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C)NC(=O)C4=CC(=CC=C4)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645285 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
819 19 6 10 3.9 CN(CCCCC(=O)NC1=CC(=C(C=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)OC)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645328 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 17 6 9 5.2 CN(C1=CC=CC(=C1)CC(=O)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645337 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
883 18 6 10 5.7 CC(CC1=C(C=CC(=C1)CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)F)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645346 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
895 19 6 10 5.6 CC(CC1=C(C=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)OC)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645314 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC=C(C=C1)CNC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645343 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645289 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
831 20 6 9 4.9 CC(CC1=CC=CC(=C1)CC(=O)NCCCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645320 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 6.1 CC(CC1=CC=CC(=C1)CCNC(=O)C2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645294 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 15 6 9 5.5 CC1=C(C=C(C=C1)C(=O)NC2=C(C=C(C=C2)CNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645293 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
823 15 6 9 5.2 CC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)C4=CC(=CC=C4)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645365 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=CC(=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645349 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=CC(=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645327 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 17 6 9 5.2 CN(C1=CC=CC(=C1)CC(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645321 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 6.1 CC(CC1=CC=CC(=C1)CCNC(=O)C2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645311 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC=C(C=C1)CNC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645295 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
839 16 6 10 4.8 CN(C1=CC=CC(=C1)C(=O)NC2=C(C=C(C=C2)CNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)OC)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3426704 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
720 14 5 9 4.0 CN(C1=CC(=C(C=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)OC)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645291 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
831 20 6 9 4.9 CC(CC1=CC=CC(=C1)CC(=O)NCCCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645298 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
823 16 6 9 5.3 CN(C1=CC=CC(=C1)C(=O)NC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645357 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
883 18 6 10 5.7 CC(CC1=CC(=C(C=C1)F)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645344 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC=C(C=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645332 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC(=CC=C1)CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645281 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
817 19 6 9 4.6 CC(CC1=CC=CC(=C1)CC(=O)NCCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645334 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 18 6 9 5.9 CC1=C(C=C(C=C1)CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)CC(C)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645359 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
789 18 6 9 4.0 CN(CCCC(=O)NC1=CC=C(C=C1)CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645317 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC=CC(=C1)CC(=O)NC2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645277 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
803 17 6 9 4.3 CC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C)NC(=O)CCCN(C)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645323 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 6.1 CC(CC1=CC=C(C=C1)CCNC(=O)C2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645307 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC=C(C=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645361 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.6 CC1=C(C=C(C=C1)C(=O)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645283 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
803 18 6 9 4.3 CC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCCCN(C)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645316 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC(=CC=C1)CNC(=O)C2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645331 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC=C(C=C1)CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645348 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
883 18 6 10 5.7 CC(CC1=C(C=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)F)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645309 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 17 6 9 5.6 CC(CC1=CC(=CC=C1)CNC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645301 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC(=CC=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3639442 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=C(C=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645353 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 5.9 CC(CC1=CC=CC(=C1)CCC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645350 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=CC(=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645282 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
817 19 6 9 4.6 CC(CC1=CC=CC(=C1)CC(=O)NCCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645356 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
895 19 6 10 5.6 CC(CC1=CC(=C(C=C1)OC)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645326 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
887 17 6 10 5.4 CN(C1=CC=CC(=C1)CC(=O)NC2=C(C=C(C(=C2)OC)CNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)Cl)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645280 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
803 18 6 9 4.5 CC(CC1=CC(=CC=C1)NC(=O)CCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645352 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=C(C=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645340 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 18 6 9 5.1 CN(C1=CC=C(C=C1)CNC(=O)CC2=CC(=CC=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645284 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
819 19 6 10 3.9 CN(CCCCC(=O)NC1=C(C=C(C=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)OC)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645351 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
879 19 6 9 6.0 CC(CC1=CC=C(C=C1)CCNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645345 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
895 19 6 10 5.6 CC(CC1=C(C=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)OC)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645342 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645302 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 16 6 9 6.1 CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)CC(C)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645292 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
823 15 6 9 5.2 CC1=C(C=C(C=C1)C(=O)NC2=CC=C(C=C2)CNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645310 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 17 6 9 6.0 CC1=C(C=C(C=C1)C(=O)NCC2=CC=CC(=C2)CC(C)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N(C)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL3645290 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
831 20 6 9 4.9 CC(CC1=CC=CC(=C1)CC(=O)NCCCCN(C)C(=O)CCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)NCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3645274 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
789 17 6 9 3.9 CC1=C(C=CC(=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCCN(C)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645287 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
803 19 6 9 4.4 CN(CCCCC(=O)NC1=CC=CC(=C1)CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645275 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
805 18 6 10 3.6 CN(CCCC(=O)NC1=C(C=C(C=C1)CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)OC)C(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3645333 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
865 18 6 9 5.6 CC(CC1=CC(=CC=C1)CNC(=O)CC2=CC=C(C=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645308 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC=C(C=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645305 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
837 16 6 9 5.7 CC(CC1=CC=C(C=C1)NC(=O)C2=CC(=CC=C2)N(C)C(=O)CCN3CCC(CC3)OC(=O)NC4=CC=CC=C4C5=CC=CC=C5)NCC(C6=C7C=CC(=O)NC7=C(C=C6)O)O
CHEMBL3645330 adrb2_human Human No 9.0 EC50 = 1 Funct
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
851 18 6 9 5.1 CN(C1=CC=C(C=C1)CC(=O)NCC2=CC=CC(=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C(=O)CCN5CCC(CC5)OC(=O)NC6=CC=CC=C6C7=CC=CC=C7
CHEMBL154370 adrb2_human Human No 9.0 EC50 = 1 Funct
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
466 11 4 4 4.5 CC1=CC=C(C=C1)CNC(=O)CC2=CC=C(C=C2)NCC(C)NCC(C3=CC(=CC=C3)Cl)O
CHEMBL1346 adrb2_cavpo Guinea pig Yes 9.0 EC50 = 1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
427 7 1 3 4.6 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
CHEMBL1682221 adrb2_cavpo Guinea pig No 9.0 EC50 = 1 Funct
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
551 10 6 6 3.7 C1=CC=C(C=C1)OC2=CC=CC(=C2)NC(=O)NC3=CC=CC(=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3099249 adrb2_cavpo Guinea pig No 9.0 EC50 = 1 Funct
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
701 18 4 9 5.7 CC(CC1=CC=C(C=C1)OCCCCCCN2C(=O)C3CCCCC3C(=N2)C4=CC(=C(C=C4)OC)OC)NCC(C5=CC(=C(C=C5)O)NC=O)O
CHEMBL1814279 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
532 19 7 8 0.2 C1=CC(=CC(=C1)NC(=O)NCC(=O)O)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O
CHEMBL1800656 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
458 13 3 6 2.8 CCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807827 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC(=CC(=C1)Cl)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1256786 adrb2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL3298986 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
503 11 6 7 2.8 CC(C)(COC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)N
CHEMBL577917 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
499 11 7 7 -0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCN=C(N)N)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1256786 adrb2_human Human Yes 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1945038 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
479 12 5 7 2.6 C1=CC=NC(=C1)CCCNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1947153 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
504 9 4 6 4.1 C1CN(CCC1C2=CC=CC=C2)CC3=CC=CC(=C3)CCNCC(C4=C5C(=C(C=C4)O)NC(=O)S5)O
CHEMBL1945044 adrb2_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
480 11 5 7 2.8 COC1=CC=CC(=C1)CNCC2=CC=CC(=C2)CCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL307647 adrb2_human Human No 9.0 EC50 = 1 Funct
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
527 3 2 5 3.3 COC1=C(C=C(C=C1I)CC2C3=C(CCN2)N=C(S3)N)I
CHEMBL230490 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
517 11 5 5 4.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL577702 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
457 10 6 7 0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1683938 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1683932 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
613 15 5 7 5.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL230490 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
517 11 5 5 4.3 CC(CC1=CC=CC(=C1)CC(=O)NCC2=CC(=C(C=C2)Cl)Cl)NCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL577702 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
457 10 6 7 0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1683938 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
641 17 5 7 6.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1683932 adrb2_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
613 15 5 7 5.2 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCCCCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL583235 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
514 12 7 8 -0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL570834 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
597 13 6 9 0.5 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN2CCN(CC2)C)NCC(C3=C4C(=C(C=C3)O)NC(=O)CO4)O
CHEMBL186271 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
618 12 4 10 4.8 CC(CC1=CNC2=C1C=CC=C2OS(=O)(=O)C3=CC=CS3)NCC(C4=CC(=CC=C4)NS(=O)(=O)C5=CC=CS5)O
CHEMBL583235 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
514 12 7 8 -0.3 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL570834 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
597 13 6 9 0.5 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNC(=O)CN2CCN(CC2)C)NCC(C3=C4C(=C(C=C3)O)NC(=O)CO4)O
CHEMBL186271 adrb2_human Human No 8.9 EC50 = 1.2 Funct
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
618 12 4 10 4.8 CC(CC1=CNC2=C1C=CC=C2OS(=O)(=O)C3=CC=CS3)NCC(C4=CC(=CC=C4)NS(=O)(=O)C5=CC=CS5)O
CHEMBL1940830 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940833 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 6 6 2.5 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)O
CHEMBL1940830 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
423 11 6 6 2.7 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)O
CHEMBL1940833 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
460 10 6 6 2.5 C1=CC=C(C=C1)C(CNC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)O
CHEMBL1807869 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC(=CC(=C1)Cl)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807869 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
482 13 5 7 3.2 C1=CC(=CC(=C1)Cl)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL3426707 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 15 6 9 4.2 COC1=C(C=C(C=C1)CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL3426707 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
720 15 6 9 4.2 COC1=C(C=C(C=C1)CCNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6
CHEMBL1945296 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
547 12 5 6 4.9 C1=CC(=CC(=C1)CNCCC2=C(C=CC=C2Cl)Cl)CCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL1945296 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
547 12 5 6 4.9 C1=CC(=CC(=C1)CNCCC2=C(C=CC=C2Cl)Cl)CCCNCC(C3=C4C(=C(C=C3)O)NC(=O)S4)O
CHEMBL3290991 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
423 11 5 6 3.8 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL3290989 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL3290991 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
423 11 5 6 3.8 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL3290989 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL1256786 adrb2_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1683931 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
557 11 5 7 3.5 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL603274 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
391 6 4 5 2.4 CC(C)(CC1=CC=C(C=C1)Cl)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL189081 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
613 12 4 10 3.7 CC(CC1=CNC2=C1C=CC=C2OS(=O)(=O)C3=CN=CC=C3)NCC(C4=CC(=CC=C4)NS(=O)(=O)C5=CC=CS5)O
CHEMBL1363 adrb2_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1683931 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
557 11 5 7 3.5 C1CN(CCC1OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)CCCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL603274 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
391 6 4 5 2.4 CC(C)(CC1=CC=C(C=C1)Cl)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL189081 adrb2_human Human No 8.9 EC50 = 1.3 Funct
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
613 12 4 10 3.7 CC(CC1=CNC2=C1C=CC=C2OS(=O)(=O)C3=CN=CC=C3)NCC(C4=CC(=CC=C4)NS(=O)(=O)C5=CC=CS5)O
CHEMBL603271 adrb2_human Human Yes 8.9 EC50 = 1.4 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
386 7 4 6 1.8 CC(C)(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL600617 adrb2_human Human No 8.9 EC50 = 1.4 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC=CC=C1C(F)(F)F)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL603271 adrb2_human Human Yes 8.9 EC50 = 1.4 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
386 7 4 6 1.8 CC(C)(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL600617 adrb2_human Human No 8.9 EC50 = 1.4 Funct
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
424 6 4 8 2.7 CC(C)(CC1=CC=CC=C1C(F)(F)F)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
CHEMBL1095777 adrb2_human Human Yes 8.8 EC50 = 1.5 Funct
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
393 6 4 4 3.3 CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
CHEMBL576848 adrb2_human Human No 8.8 EC50 = 1.5 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
399 7 4 5 2.9 CC(C)C1=CC=C(C=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL1095777 adrb2_human Human Yes 8.8 EC50 = 1.5 Funct
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
393 6 4 4 3.3 CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
CHEMBL576848 adrb2_human Human No 8.8 EC50 = 1.5 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
399 7 4 5 2.9 CC(C)C1=CC=C(C=C1)CC(C)(C)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL181964 adrb2_human Human No 8.8 EC50 = 1.5 Funct
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
458 11 4 6 3.9 CC(CC1=CNC2=C1C=CC=C2OS(=O)(=O)C)NCC(C3=CC(=CC=C3)NCC(=C)C)O
CHEMBL1419122 adrb2_human Human Yes 8.8 EC50 = 1.5 Funct
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
447 10 1 6 4.3 C=CCN1C(=NN=C1SCC(=O)C2=CC=C(C=C2)Cl)CCNC(=O)C3=CC=CS3
CHEMBL1256786 adrb2_cavpo Guinea pig Yes 8.8 EC50 = 1.6 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL1256786 adrb2_cavpo Guinea pig Yes 8.8 EC50 = 1.6 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
344 8 4 5 1.8 CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O
CHEMBL111775 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
430 12 4 6 2.2 C1=CC=C(C=C1)CCOCCC(=O)NCCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL1800659 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
486 15 3 6 3.6 CCCCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL111775 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
430 12 4 6 2.2 C1=CC=C(C=C1)CCOCCC(=O)NCCNCCC2=C3C(=C(C=C2)O)NC(=O)S3
CHEMBL1800659 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
486 15 3 6 3.6 CCCCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1807829 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
516 13 5 7 3.8 C1=CC(=C(C(=C1)Cl)Cl)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807871 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
516 13 5 7 3.8 C1=CC(=C(C(=C1)Cl)Cl)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807829 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
516 13 5 7 3.8 C1=CC(=C(C(=C1)Cl)Cl)CCNCCCSCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1807871 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
516 13 5 7 3.8 C1=CC(=C(C(=C1)Cl)Cl)CCNCCSCCCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1800659 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
486 15 3 6 3.6 CCCCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL1800659 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
486 15 3 6 3.6 CCCCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC=CC=C3
CHEMBL3426700 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.9 COC1=C(C=CC(=C1)C(=O)NCCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3426700 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
706 14 6 9 3.9 COC1=C(C=CC(=C1)C(=O)NCCN2CCC(CC2)OC(=O)NC3=CC=CC=C3C4=CC=CC=C4)CNCC(C5=C6C=CC(=O)NC6=C(C=C5)O)O
CHEMBL3298762 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
579 13 6 7 4.1 C1=CC=C(C=C1)C(=O)NCCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298897 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
544 12 6 8 2.5 C1CN(CCN1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298762 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
579 13 6 7 4.1 C1=CC=C(C=C1)C(=O)NCCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL3298897 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
544 12 6 8 2.5 C1CN(CCN1)CCOC2=CC=C(C=C2)NC3=CC=C(C=C3)CCNCC(C4=C5C=CC(=O)NC5=C(C=C4)O)O
CHEMBL1945035 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)CNCCC4=CC=CC=C4F
CHEMBL1945035 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
482 11 5 7 3.4 C1=CC=C(C(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O)CNCCC4=CC=CC=C4F
CHEMBL475237 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
509 18 5 8 2.4 C1=CC(=CC(=C1)CS(=O)(=O)N)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O
CHEMBL475237 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
509 18 5 8 2.4 C1=CC(=CC(=C1)CS(=O)(=O)N)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O
CHEMBL1940820 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
457 11 6 6 3.4 C1=CC(=CC=C1CCNCC(C2=CC(=C(C=C2)O)CO)O)NCC(C3=CC=C(C=C3)Cl)O
CHEMBL1940820 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
457 11 6 6 3.4 C1=CC(=CC=C1CCNCC(C2=CC(=C(C=C2)O)CO)O)NCC(C3=CC=C(C=C3)Cl)O
CHEMBL3099659 adrb2_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
331 8 4 5 2.8 CCC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC(=C2)O)O)O
CHEMBL565686 adrb2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
433 7 4 5 3.4 CC(C)(CC1=CC=C(C=C1)C2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)CO4)O
CHEMBL565686 adrb2_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
433 7 4 5 3.4 CC(C)(CC1=CC=C(C=C1)C2=CC=CC=C2)NCC(C3=C4C(=C(C=C3)O)NC(=O)CO4)O
CHEMBL585751 adrb2_human Human No 8.7 EC50 = 1.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
579 15 7 10 -2.2 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNCCCS(=O)(=O)O)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL585751 adrb2_human Human No 8.8 EC50 = 1.8 Funct
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
579 15 7 10 -2.2 CC(C)(CC1=CC=C(C=C1)NC(=O)CCCNCCCS(=O)(=O)O)NCC(C2=C3C(=C(C=C2)O)NC(=O)CO3)O
CHEMBL2335410 adrb2_cavpo Guinea pig No 8.7 EC50 = 2.0 Funct
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
564 14 5 8 3.7 COC1=C(C=C(C=C1)C(=O)NC2=C(C=NC=C2Cl)Cl)OCCCCCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL3290997 adrb2_cavpo Guinea pig No 8.7 EC50 = 2.0 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL3290999 adrb2_cavpo Guinea pig Yes 8.7 EC50 = 2.0 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3290997 adrb2_cavpo Guinea pig No 8.7 EC50 = 2.0 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
485 11 5 6 5.0 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O)C4=CC=CC=C4
CHEMBL3290999 adrb2_cavpo Guinea pig Yes 8.7 EC50 = 2.0 Funct
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
522 10 5 6 4.8 COC1=C(C=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C5=CC=CC=C5
CHEMBL3298327 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
460 10 5 6 3.5 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL3298327 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
460 10 5 6 3.5 CCOC1=CC=C(C=C1)NC2=CC=C(C=C2)CCNCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O
CHEMBL1945292 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
418 11 5 7 1.2 COCCNCC1=CC=CC(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1945292 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
418 11 5 7 1.2 COCCNCC1=CC=CC(=C1)CCNCC(C2=C3C(=C(C=C2)O)NC(=O)S3)O
CHEMBL1084655 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
497 17 5 9 1.1 C1=CC(=CC=C1COCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O)S(=O)(=O)N
CHEMBL1084655 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
497 17 5 9 1.1 C1=CC(=CC=C1COCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O)S(=O)(=O)N
CHEMBL3290988 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
455 10 5 5 5.1 C1=CC=C(C=C1)C2=CC(=CC=C2)NC3=CC=C(C=C3)CCNCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL3290988 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
455 10 5 5 5.1 C1=CC=C(C=C1)C2=CC(=CC=C2)NC3=CC=C(C=C3)CCNCC(C4=CC(=C(C=C4)O)CO)O
CHEMBL1940818 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
437 11 5 6 2.9 CN(CC(C1=CC=CC=C1)O)C2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1940821 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
441 11 6 7 2.8 C1=CC(=CC=C1CCNCC(C2=CC(=C(C=C2)O)CO)O)NCC(C3=CC=C(C=C3)F)O
CHEMBL1940818 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
437 11 5 6 2.9 CN(CC(C1=CC=CC=C1)O)C2=CC=C(C=C2)CCNCC(C3=CC(=C(C=C3)O)CO)O
CHEMBL1940821 adrb2_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
441 11 6 7 2.8 C1=CC(=CC=C1CCNCC(C2=CC(=C(C=C2)O)CO)O)NCC(C3=CC=C(C=C3)F)O
CHEMBL3265168 adrb2_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
579 17 3 7 4.4 CCN(CC)CCN(CCNCCC1=C2C(=C(C=C1)O)NC(=O)S2)C(=O)CCOCCC3=CC4=CC=CC=C4C=C3
CHEMBL3265164 adrb2_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activ