Table 6.
Study | Compound | Assays* | Activity | Lit. no.‡ | Ref. |
---|---|---|---|---|---|
Muller (1997) | IG-47 | Lipogenesis | 15.5-fold stimulation, EC50 = 1.0 μM |
PIG-P | [37] |
Muller (1998) | 65–75% MIR, EC50 = 2–5 μM | PIG-P | [51] | ||
Muller (2002) | 22-fold stimulation at 10 μM | YCN-PIG | [48] | ||
Muller (1997) | GPAT | 75–85% MIR, EC50 = 3–5 μM | PIG-P | [37] | |
Muller (1998) | 85% MIR at 5 μM | PIG-P | [51] | ||
Muller (1997) | Glucose transport | 15-fold increase, EC50 = 1.0–1.5 μM |
PIG-P | [37] | |
Kessler (1998) | sixfold stimulation at 10 μM | PIG-P | [54] | ||
Muller (1997) | GLUT4 translocation | 85% MIR, EC50 = 2–3 μM | PIG-P | [37] | |
Muller (1997) | Glycogenesis | 75–90% MIR, EC50 = 8–10 μM | PIG-P | [37] | |
Muller (2002) | eightfold stimulation at 10 μM | YCN-PIG | [48] | ||
Muller (1997) | GS stimulation | 2.8-fold stimulation, EC50 = 8.0 μM |
PIG-P | [37] | |
Muller (2002) | fourfold stimulation at 10 μM | YCN-PIG | [48] | ||
Muller (2002) | Glycerol-3-phosphate acyltransferase activity |
sixfold stimulation at 10 μM | YCN-PIG | [48] | |
Muller (1997) | cAMP-dependent protein kinase activity |
70% MIR, EC50 = 0.3–0.5 μM | PIG-P | [37] | |
Muller (1997) | Lipolysis | 70% inhibition, EC50 = 0.5–0.8 μM |
PIG-P | [37] | |
Muller (2002) | 95% inhibition at 10 μM | YCN-PIG | [48] | ||
Kessler (1998) | PI-3 kinase activity | 2.3-fold stimulation, | 76% MIR PIG-P | [54] | |
Muller (2002) | Radiolabeled study with hcDIGs of adipocyte plasma membranes |
Specific interaction with hcDIGs, Kd 30–100 nM, Bmax = 5–10 pmol/mg hcDIGs |
YCN-PIG | [74] | |
Muller (1998) | Tyrosine phosphorylation of caveolin |
80% MIR at 10 μM, EC50 = 1–2 μM |
PIG-P | [51] | |
Kessler (1998) | Tyrosine | 2.3-fold stimulation, 44% MIR | PIG-P | [54] | |
Muller (2002) | phosphorylation of IRS-1 | 24-fold stimulation at 5 nM | YCN-PIG | [48] | |
| |||||
Frick (1998) | IG-48 | Lipogenesis | Activity ‘A’§ | 2 | [45] |
Frick (1999) | 10% MIR, EC50 = 20 μM | O | [101] | ||
Glucose transport | 5% MIR, EC50 = 50 μM | ||||
| |||||
Frick (1998) | IG-49 | Lipogenesis | Activity ‘A’§ | 3 | [45] |
| |||||
Frick (1998) | IG-50 | Lipogenesis | Activity ‘A’§ | 4 | [45] |
Frick (1999) | 18% MIR, EC50 = 20 μM | 1 | [101] | ||
Glucose transport | 14% MIR, EC50 = 50 μM | ||||
| |||||
Frick (1998) | IG-51 | Lipogenesis | Activity ‘B’§ | 5 | [45] |
| |||||
Frick (1998) | IG-52 | Lipogenesis | Activity ‘B’§ | 6 | [45] |
| |||||
Frick (1998) | IG-53 | Lipogenesis | Activity ‘B’§ | 9 | [45] |
| |||||
Frick (1998) | IG-54 | Lipogenesis | Activity ‘B’§ | 10 | [45] |
Frick (1999) | 33% MIR, EC50 = 20 μM | D | [101] | ||
Glucose transport | 18% MIR, EC50 = 18 μM | ||||
| |||||
Frick (1998) | IG-55 | Lipogenesis | Activity ‘B’§ | 11 | [45] |
| |||||
Frick (1998) | IG-56 | Lipogenesis | Activity ‘C’§ | 14 | [45] |
Frick (1999) | 48% MIR, EC50 = 15 μM | R | [101] | ||
Glucose transport | 19% MIR, EC50 = 10 μM | ||||
| |||||
Frick (1998) | IG-57 | Lipogenesis | Activity ‘C’§ | 15 | [45] |
Frick (1999) | 50% MIR, EC50 = 15 μM | S | [101] | ||
Glucose transport | 34% MIR, EC50 = 20 μM | ||||
| |||||
Frick (1998) | IG-58 | Lipogenesis | Activity ‘C’§ | 16 | [45] |
Frick (1999) | 72% MIR, EC50 = 12 μM | T | [101] | ||
Glucose transport | 30% MIR, EC50 = 10 μM | ||||
| |||||
Frick (1998) | IG-59 | Lipogenesis | Activity ‘D’§ | 17 | [45] |
Frick (1999) | 80% MIR, EC50 = 15 μM | U | [101] | ||
Glucose transport | 34% MIR, EC50 = 15 μM | ||||
| |||||
Frick (1998) | IG-60 | Lipogenesis | Activity ‘D’§ | 18 | [45] |
Frick (1999) | 83% MIR, EC50 = 15 μM | V | [101] | ||
Glucose transport | 48% MIR, EC50 = 15 μM | ||||
| |||||
Frick (1998) | IG-61 | Lipogenesis | Activity ‘D’§ | 19 | [45] |
Frick (1999) | 86% MIR, EC50 = 10 μM | W | [101] | ||
Glucose transport | 42% MIR, EC50 = 10 μM | ||||
| |||||
Frick (1998) | IG-62 | Lipogenesis | Activity ‘B’§ | 21 | [45] |
| |||||
Frick (1998) | IG-63 | Lipogenesis | Activity ‘B’§ | 22 | [45] |
| |||||
Frick (1998) | IG-64 | Lipogenesis | Activity ‘B’§ | 25 | [45] |
| |||||
Frick (1998) | IG-65 | Lipogenesis | Activity ‘B’§ | 26 | [45] |
| |||||
Frick (1998) | IG-66 | Lipogenesis | Activity ‘B’§ | 27 | [45] |
| |||||
Frick (1998) | IG-67 | Lipogenesis | Activity ‘C’§ | 30 | [45] |
Frick (1999) | 48% MIR, EC50 = 60 μM | E | [101] | ||
Glucose transport | 34% MIR, EC50 = 30 μM | ||||
| |||||
Frick (1998) | IG-68 | Lipogenesis | Activity ‘C’§ | 31 | [45] |
Frick (1999) | 53% MIR, EC50 = 15 μM | F | [101] | ||
Glucose transport | 26% MIR, EC50 = 25 μM | ||||
| |||||
Frick (1998) | IG-69 | Lipogenesis | Activity ‘C’ § | 32 | [45] |
| |||||
Frick (1998) | IG-70 | Lipogenesis | Activity ‘C’§ | 33 | [45] |
Frick (1999) | 59% MIR, EC50 = 7 μM | A | [101] | ||
Glucose transport | 28% MIR, EC50 = 8 μM | ||||
| |||||
Frick (1998) | IG-71 | Lipogenesis | Activity ‘C’§ | 34 | [45] |
Frick (1999) | 63% MIR, EC50 = 8 μM | J | [101] | ||
Glucose transport | 21% MIR, EC50 = 3 μM | ||||
| |||||
Frick (1999) | IG-72 | Lipogenesis | Activity ‘C’§ | 35 | [45] |
Frick (1999) | 64% MIR, EC50 = 7 μM | C | [101] | ||
Glucose transport | 29% MIR, EC50 = 10 μM | ||||
| |||||
Frick (1998) | IG-73 | Lipogenesis | Activity ‘C’§ | 36 | [45] |
Frick (1999) | 72% MIR, EC50 = 8 μM | K | [101] | ||
Glucose transport | 23% MIR, EC50 = 15 μM | ||||
| |||||
Frick (1998) | IG-74 | Lipogenesis | 80% MIR at 20 μM, IC50 = 2.2 ± 0.2 μM |
37 | [45] |
Frick (1999) | 77% MIR, EC50 = 8.2 μM | B | [101] | ||
Frick (1998) | GPAT | 90% MIR, IC50 = 8.0 ± 1.1 μM | 37 | [45] | |
Glucose transport 90–95% MIR at 20 μM, IC50 = 8.3 ± 1.5 μM |
|||||
Frick (1999) | 41% MIR, EC50 = 8.1 μM | B | [101] | ||
Frick (1998) | GLUT4 translocation | 50% MIR | 37 | [45] | |
Glycogenesis 65% MIR at 20 μM, IC50 = 7.1 ± 2.0 μM |
|||||
Lipolysis | 95% MIR, IC50 = 2.5 ± 0.5 μM | ||||
Tyrosine phosphorylation of IRS-1 | 65% MIR at 10 μM | ||||
| |||||
Frick (1998) | IG-75 | Lipogenesis | Activity ‘D’§ | 38 | [45] |
Frick (1999) | 90% MIR, EC50 = 7 μM | M | [101] | ||
Glucose transport | 39% MIR, EC50 = 6 μM | ||||
| |||||
Frick (1998) | IG-76 | Lipogenesis | Activity ‘D’§ | 39 | [45] |
Frick (1999) | 84% MIR, EC50 = 7 μM | L | [101] | ||
Glucose transport | 36% MIR, EC50 = 8 μM | ||||
| |||||
Frick (1998) | IG-77 | Lipogenesis | Activity ‘D’§ | 40 | [45] |
| |||||
Frick (1998) | IG-78 | Lipogenesis | 90% MIR at 20 μM, IC50 = 2.5 ± 0.9 μM |
41 | [45] |
Frick (1999) | 96% MIR, EC50 = 3 μM | N | [101] | ||
Frick (1998) | GPAT | 90% MIR, IC50 = 3.5 ± 0.8 μM | 41 | [45] | |
Frick (1999) | Glucose transport | 90–95% MIR at 20 μM, IC50 = 3.5 ± 0.6 μM |
|||
Frick (1998) | 52% MIR, EC50 = 5 μM | N | [101] | ||
GLUT4 translocation 50% MIR | 41 | [45] | |||
Glycogenesis 70% MIR at 20 μM, IC50 = 3.3 ± 0.5 μM |
|||||
Lipolysis | 95% MIR, IC50 = 1.6 ± 0.5 μM | ||||
| |||||
Frick (1998) | IG-79 | Tyrosine phosphorylation of IRS-1 |
95% MIR at 10 μM | 45 | [45] |
Lipogenesis | Activity ‘C’§ | ||||
Tyrosine phosphorylation of IRS-1 |
55% MIR at 10 μM | ||||
| |||||
Frick (1998) | IG-80 | Lipogenesis | Activity ‘C’§ | 46 | [45] |
Details of assays (in alphabetical order) are provided in the text.
The number assigned to this compound in the cited publication.
Note: for Muller’s SAR study [45] aggregate activities were reported as follows: “A”, MIR < 20%; “B”, MIR 20–49%, EC20 25–200 μM; “C”, MIR 50–80%, EC50 10–100 μM; “D”, MIR > 80%, EC50 3–30 μM.
Lit. no.: Literacy number; MIR: Maximal insulin response.