Partial List of Benzoylindoles

The affinity values are included just for information purposes.  Note that these are from different types of studies; so one compares apples to oranges unless using values from similar types of assays.

 

       

 

Name R1 R2 R3 R4 R5 R6 R7 CB1 K1 CB2 K1 CB1/CB2 
AM1298 methyl-2-(1-Me-piperidinyl) H I H H     2.8 2.9 0.97
AM661 methyl-2-(1-Me-piperidinyl) Methyl I H H     34 34 1.00
Deng 2.20 methyl-2-(1-Me-piperidinyl) Methyl H I H     2900 9600 0.30
Deng 2.17 methyl-2-(1-Me-piperidinyl) Methyl H H I     1800 790 2.28
Pravadoline ethyl-4-morpholino Methyl H H Methoxy          
AM630 ethyl-4-morpholino Methyl H H Methoxy 6-I   995 335 2.97
AM679 Pentyl H I H H     13.9 49.6 0.28
Deng 2.23 Butyl Methyl I H H     272 281 0.97
Deng 2.24 Pentyl Methyl I H H     47.2 38.6 1.22
Deng 2.25 Hexyl Methyl I H H     332 693 0.48
Deng 2.26 Heptyl Methyl I H H     1603 1511 1.06
Deng 2.31 5-Acetyl-pentyl Methyl I H H     2279 1019 2.24
Deng 2.33 5-Hydroxy-pentyl Methyl I H H     4850 1972 2.46
Deng 2.35 5-OTs-pentyl Methyl I H H     1024 2968 0.35
Deng 2.37 5-Azido-pentyl Methyl I H H     22.4 62.7 0.36
Deng 2.39 5-NCS-pentyl Methyl I H H     195 29.5 6.61
Deng 2.41 5-Iodo-pentyl Methyl I H H     116.5 46.2 2.52
Deng 2.27 Pentyl H I H H     13.5 49.5 0.27
Deng 2.30 5-Acetyl-pentyl H I H H     2656 1519 1.75
Deng 2.32 5-Hydroxy-pentyl H I H H     835 526 1.59
Deng 2.34 5-OTs-pentyl H I H H     1306 1116 1.17
Deng 2.36 5-Azido-pentyl H I H H     121 128 0.95
Deng 2.38 5-NCS-pentyl H I H H     106 110 0.96
Deng 2.40 5-Iodo-pentyl H I H H     135.8 314.7 0.43
Deng 2.44 Pentyl H I H H & 5-NO2     98.9 22.9 4.32
Deng 2.45 Pentyl H I H H & 5-NH2     63.6 88.9 0.72
Deng 2.46 Pentyl H I H H & 5-N3     116.9 45.2 2.59
Deng 2.47 Pentyl H I H H & 5-I     105.1 70.3 1.50
Deng 2.48 Pentyl H I H H & 5-NCS     3632 2040 1.78
Deng 2.21 methyl-2-(1-Me-piperidinyl) Methyl I H H     33.6 33.9 0.99
Deng 2.49 methyl-2-(1-Me-piperidinyl) Methyl I H H 6-NO2   40 80 0.50
Deng 2.50 methyl-2-(1-Me-piperidinyl) Methyl I H H 6-NH2   63.6 20.3 3.13
AM1216 methyl-2-(1-Me-piperidinyl) Methyl I H H 6-N3   40.7 22 1.85
Deng 2.52 methyl-2-(1-Me-piperidinyl) Methyl I H H 6-I   21 2.92 7.19
AM1215 methyl-2-(1-Me-piperidinyl) Methyl I H H 6-NCS   21 25.3 0.83
AM2233 methyl-2-(1-Me-piperidinyl) H I H H     3.4 7.6 0.45
AM1241 methyl-2-(1-Me-piperidinyl) H I H H & 5-NO2     548.4 1.6 342.75
Deng 4.2 methyl-2-(1-Me-piperidinyl) Methyl I H H & 5-NO2     2133 41.8 51.03
Deng 4.3 methyl-2-(1-Me-piperidinyl) H I H H & 5-NO2 6-I   199 17.5 11.37
Deng 4.4 methyl-2-(1-Me-piperidinyl) H F H H & 5-NO2     460 83.1 5.54
Deng 4.5 methyl-2-(1-Me-piperidinyl) H I H H & 5-N(Me)2     48.6 33 1.47
Deng 4.6 methyl-2-(1-Me-piperidinyl) H I H H & 5-I     24.8 5.4 4.59
Deng 4.7 methyl-2-(1-Me-piperidinyl) H I H H & 5-NH2     11.7 9.8 1.19
Deng 4.8 methyl-2-(1-Me-piperidinyl) H I H H & 5-N3     48.3 41.8 1.16
Deng 4.9 methyl-2-(1-Me-piperidinyl) H I H H & 5-NCS     64.8 29.9 2.17
AM694 5-Fluoro-pentyl H I H H     0.08 1.44 0.06
Deng 7.8 5-Fluoro-pentyl Methyl I H H     5.97 3.8 1.57
TEDA96-11 methyl-2-(1-Me-piperidinyl) Methyl H H Methoxy          
TEDA96-12 3-(1-Me-piperidinyl) Methyl H H Methoxy          
TEDA96-13 ethyl-2-(1-Me-piperidinyl) Methyl H H Methoxy          
TEDA96-14 methyl-3-(1-Me-piperidinyl) Methyl H H Methoxy          
TEDA96-15 4-(1-Me-piperidinyl) Methyl H H Methoxy          
TEDA96-16 methyl-2-(1-Me-pyrrolidinyl) Methyl H H Methoxy          
TEDA96-17 methyl-2-(1-Me-pyrrolidinyl) Methyl H H Methoxy          
TEDA96-18 methyl-2-(1-Me-pyrrolidinyl) Methyl H H Methoxy          
TEDA96-19 Me-2-(1,4-di-Me-piperazinyl) Methyl H H Methoxy          
TEDA96-20 methyl-3-(4-Me-morpholinyl) Methyl H H Methoxy          
TEDA96-21 methyl-2-(4-Me-morpholinyl) Methyl H H Methoxy          
TEDA96-22 3-(4-Me-thiomorpholinyl) Methyl H H Methoxy          
TEDA96-23 3-(4-Me-thiomorpholinyl)oxide Methyl H H Methoxy          
TEDA96-24 2-pyrrolidinyl Methyl H H Methoxy          
TEDA96-25 Me-2-(1-Et-pyrrolidinyl) Methyl H H Methoxy          
TEDA96-26 methyl-2-(1-Me-piperidinyl) H H H Methoxy          
TEDA96-27 methyl-2-(1-Me-pyrrolidinyl) H H H Methoxy          
MAE95-18 ethyl-4-morpholino Methyl H H H          
MAE95-19 ethyl-4-morpholino Methyl Methoxy H H          
MAE95-20 ethyl-4-morpholino Methyl H Methoxy H          
MAE95-21 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-22 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-23 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-24 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-25 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-26 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-27 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-28 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-29 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-30 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-31 ethyl-4-morpholino Methyl H H Methoxy          
MAE95-32 H Methyl H H Methoxy          
MAE95-33 CH2-CO2H Methyl H H Methoxy          
MAE95-34 (CH2)2-OH Methyl H H Methoxy          
MAE95-35 (CH2)2-NH2 Methyl H H Methoxy          
MAE95-36 (CH2)2-NMe2 Methyl H H Methoxy          
MAE95-37 (CH2)2-NEt2 Methyl H H Methoxy          
MAE95-38 (CH2)2-piperidinyl Methyl H H Methoxy          
MAE95-39 (CH2)2-pyrrolidinyl Methyl H H Methoxy          
MAE95-40 (CH2)2-piperazinyl Methyl H H Methoxy          
MAE95-41 (CH2)2-4-Me-piperazinyl Methyl H H Methoxy          
MAE95-42 (CH2)2-thiomorpholino Methyl H H Methoxy          
MAE95-43 (CH2)2-thiomorpholino-oxide Methyl H H Methoxy          
MAE95-44 (CH2)2-thiomorpholinodioxide Methyl H H Methoxy          
MAE95-45 propyl-4-morpholino Methyl H H Methoxy          
MAE95-46 butyl-4-morpholino Methyl H H Methoxy          
MAE95-47 (CH2)2OH Methyl H H Methoxy          
MAE95-48 (CH2)2OH Methyl H H Methoxy          
MAE95-49 (CH2)2OH H H H Methoxy          
MAE95-50 (CH2)2OH Methyl H H Methoxy          
MAE95-51 (CH2)2OH Methyl H H Methoxy          
MAE95-52 (CH2)2OH Methyl H H Methoxy          
MAE95-53 (CH2)2OH Methyl H H Methoxy          
MAE95-54 ethyl-4-morpholino H H H Methoxy          
MAE95-55 ethyl-4-morpholino H H H Methoxy          
MAE95-56 ethyl-4-morpholino H H H Methoxy          
MAE95-57 ethyl-4-morpholino Ethyl H H Methoxy          
MAE95-58 ethyl-4-morpholino F H H Methoxy          
MAE95-59 ethyl-4-morpholino Cl H H Methoxy          
MAE95-60 ethyl-4-morpholino CN H H Methoxy          
MAE95-61 ethyl-4-morpholino OH H H Methoxy          
MAE95-62 ethyl-4-morpholino Methyl Methyl H H          
MAE95-63 ethyl-4-morpholino Methyl H Methyl H          
MAE95-64 ethyl-4-morpholino Methyl H H Methyl          
MAE95-65 ethyl-4-morpholino Methyl Hydroxy H H          
MAE95-66 ethyl-4-morpholino Methyl H H Hydroxy          
MAE95-67 ethyl-4-morpholino Methyl F H H          
MAE95-68 ethyl-4-morpholino Methyl H F H          
MAE95-69 ethyl-4-morpholino Methyl H H F          
MAE95-70 ethyl-4-morpholino Methyl Cl H H          
MAE95-71 ethyl-4-morpholino Methyl H Cl H          
MAE95-72 ethyl-4-morpholino Methyl H H Cl          
MAE95-73 ethyl-4-morpholino Methyl CN H H          
MAE95-74 ethyl-4-morpholino Methyl H CN H          
MAE95-75 ethyl-4-morpholino Methyl H H CN          
MAE95-76 ethyl-4-morpholino Methyl H H Ethyl          
MAE95-77 ethyl-4-morpholino Methyl H H Propyl          
MAE95-78 ethyl-4-morpholino Methyl H H C(CH3)3          
MAE95-79 ethyl-4-morpholino Methyl H H Phenyl          
MAE95-80 ethyl-4-morpholino Methyl Methyl H H 6-Methyl        
MAE95-81 ethyl-4-morpholino Methyl Methyl H H 5-Methyl        
MAE95-82 ethyl-4-morpholino Methyl H Methyl H 5-Methyl        
MAE95-83 ethyl-4-morpholino Methyl H Methyl Methyl