Table 1 Degradation of endogenous TEAD1, TEAD4 and cIAP1 with IPD hits and negative controls
From: Expanding the toolbox to develop IAP-based degraders of TEAD transcription factors
Compound | Description | NCI-H2052 (TEAD1) | NCI-H2052 (TEAD4) | NCI-H2052 (cIAP1) | NCI-H226 (TEAD1) | ||||
|---|---|---|---|---|---|---|---|---|---|
DC50 (nM) | Dmax (%) | DC50 (nM) | Dmax (%) | DC50 (nM) | Dmax (%) | DC50 (nM) | Dmax (%) | ||
VT-107 | TEAD binder | 3 | 21 | - | - | - | - | - | - |
A262 | TEAD binder | 800 | 36 | - | - | - | - | - | - |
A341 | TEAD binder | 2600 | 38 | - | - | - | - | - | - |
A232 A230 A231 | ALP1 IPD hit ALP1 IAP neg. control ALP1 TEAD neg. control | 14 970 4100 | 32 45 40 | - - - | - | 270 240 530 | 88 36 95 | - - - | - - - |
A531 A557 A423 | ALP2 IPD hit ALP2 IAP neg. control ALP2 TEAD neg. control | 170* 140 560 | 55* 41 23 | 1100 - - | 33 - - | 20 150 23 | 94 17 96 | 77 370 930 | 53 42 29 |
A538 A559 A561 | XB2 IPD hit XB2 IAP neg. control XB2 TEAD neg. control | 44# 1500 630 | 42# 37 10 | 510 - - | 9 - - | 39 920 360 | 100 7 97 | 76 780 1100 | 38 27 17 |
