Table. 3 Binary and ternary affinities for sfBRD3 and sfVBC ligands and PROTACs
From: Pioneering protein degradation for agricultural applications
sfBRD3 Binary Affinity | sfVBC Binary Affinity | sfVBC + sfBRD3 Ternary Affinity | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LD | SPR | LD | SPR | AlphaLISA | SPR | IVQ | ||||||||||||
Cmpd # | Type | Ki (nM) | KD (nM) | ka (1/Ms) | kd (1/s) | t1/2 (s) | Ki (nM) | KD (nM) | ka (1/Ms) | kd (1/s) | t1/2 (s) | KD,app (nM) | KD,ternary (nM) | ka (1/Ms) | kd (1/s) | t1/2 (s) | α | Y/N |
1 | sfVBC Ligand | NB | NB | NB | NB | NB | 370 | 210 | 1.1E + 06 | 2.3E-01 | 3.0 | NB | NB | NB | NB | NB | NB | No |
28 | sfVBC(-) Ligand | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
5 | sfBRD3 Ligand | 410 | 290 | 9.6E + 05 | 2.7E-01 | 2.5 | ND | NB | NB | NB | NB | ND | NB | NB | NB | NB | NB | ND |
6 | sfBRD3 Ligand | 34 | 1.2 | 1.1E + 07 | 1.3E-02 | 53 | ND | NB | NB | NB | NB | ND | NB | NB | NB | NB | NB | ND |
7 | sfBRD3 Ligand | 52 | 6.8 | 8.6E + 06 | 5.8E-02 | 12 | ND | NB | NB | NB | NB | ND | NB | NB | NB | NB | NB | ND |
8 | sfBRD3 Vestigial | 240 | 70 | 9.8E + 05 | 6.9E-02 | 10 | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
9 | sfBRD3 Vestigial | 260 | 0.9 | 1.3E + 07 | 1.1E-02 | 61 | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
10 | sfBRD3 Vestigial | 220 | 23 | 1.1E + 06 | 2.4E-02 | 29 | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
21 | sfBRD3-sfVBC PROTAC | 100 | 9.4 | 3.4E + 06 | 3.2E-02 | 22 | 77 | 91 | 1.2E + 06 | 1.1E-01 | 6.2 | <33 | 8.9 | 3.1E + 05 | 2.8E-03 | 250 | 10 | Yes |
22 | sfBRD3-sfVBC PROTAC | 79 | 10 | 1.3E + 06 | 1.4E-02 | 51 | 81 | 120 | 3.4E + 05 | 4.0E-02 | 18 | 51 | 32 | 4.4E + 05 | 1.4E-02 | 49 | 3.7 | Yes |
23 | sfBRD3-sfVBC PROTAC | 140 | 1.2 | 6.8E + 06 | 8.5E-03 | 82 | 45 | 69 | 2.3E + 06 | 1.6E-01 | 4.3 | 88 | 79 | 4.5E + 05 | 3.6E-02 | 20 | 0.9 | Yes |
24 | sfBRD3-sfVBC PROTAC | 110 | 12 | 3.4E + 05 | 3.9E-03 | 180 | 430 | 850 | 1.9E + 04 | 1.6E-02 | 44 | 47 | 25 | 8.6E + 05 | 2.2E-02 | 32 | 33 | Yes |
25 | sfBRD3-sfVBC(-) PROTAC | 100 | 12 | 1.9E + 06 | 2.3E-02 | 31 | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
26 | sfBRD3-sfVBC(-) PROTAC | 95 | 9.7 | 1.1E + 06 | 1.1E-02 | 64 | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | NB | No |
