Bioactivity Comments

Combined anti-PD-L1+anti-CTLA-4 therapy has shown benefits over anti-PD-L1 monotherapy in head and neck cancer. Compared to monotherapy, the combination approach is reported to induce more efficient CD4+ T cell trafficking from lymph nodes to tumours and to promote expansion toward T helper 1 phenotype [4].

Natural/Endogenous Targets
Target programmed cell death 1 (CD279)

Selectivity at other protein targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference programmed cell death 1 (CD279) Hs None Binding - - - ⤷

Other ligands which bind to or alter the activity of this ligand
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Ligand Sp. Type Action Value Parameter Concentration range (M) Reference atezolizumab Hs Antibody Binding 9.0 – 10.0 pKd - 9 ⤷ pKd 9.0 – 10.0 (Kd 1x10-9 – 1x10-10 M) [9] cosibelimab Monkey Antibody Binding 9.3 pKd - 1 ⤷ pKd 9.3 (Kd 5.6x10-10 M) [1] cosibelimab Hs Antibody Binding 9.1 pKd - 1 ⤷ pKd 9.1 (Kd 8.5x10-10 M) [1] durvalumab Hs Antibody Binding 8.7 pKd - 17 ⤷ pKd 8.7 (Kd 2x10-9 M) [17] envafolimab Hs Antibody Binding 8.5 pKd - 26 ⤷ pKd 8.5 (Kd 3x10-9 M) [26] X14 Hs Inhibitor Binding 7.8 pKd - 24 ⤷ pKd 7.8 (Kd 1.462x10-8 M) [24] S4-1 Hs Inhibitor Binding 7.2 pKd - 21 ⤷ pKd 7.2 (Kd 7.136x10-8 M) [21] Description: Binding affinity for hPD-L1 using a microscale thermophoresis (MST) assay PD-L1 inhibitor D6 [PMID: 40153736] Hs Inhibitor Binding 6.6 pKd - 14 ⤷ pKd 6.6 (Kd 2.3x10-7 M) [14] Description: Binding affinity for dimeric hPD-L1 X14 Mm Inhibitor Binding 6.4 pKd - 24 ⤷ pKd 6.4 (Kd 3.92x10-7 M) [24] EP26 Mm Inhibitor Binding 6.3 pKd - 25 ⤷ pKd 6.3 (Kd 5.2x10-7 M) [25] Description: Binding affinity for mouse PD-L1 determined by SPR assay. EP26 Hs Inhibitor Binding 6.2 pKd - 25 ⤷ pKd 6.2 (Kd 5.8x10-7 M) [25] Description: Binding affinity for human PD-L1 determined by SPR assay. avelumab Hs Antibody Binding 10.1 pIC50 - 16 ⤷ pIC50 10.1 (IC50 7.1x10-11 M) [16] Description: Measuring inhibition of PD-1 binding to PD-L1. BMS-1166 Hs Inhibitor Binding 8.9 pIC50 - 2,8 ⤷ pIC50 8.9 (IC50 1.4x10-9 M) [2,8] Description: Measured in a PD-1/PD-L1 homogenous time-resolved fluorescence (HTRF) binding assay. BMS-1001 Hs Inhibitor Binding 8.6 pIC50 - 2 ⤷ pIC50 8.6 (IC50 2.25x10-9 M) [2] Description: Measured in a PD-1/PD-L1 homogenous time-resolved fluorescence (HTRF) binding assay. S4-1 Hs Inhibitor Inhibition 8.2 pIC50 - 21 ⤷ pIC50 8.2 (IC50 6.1x10-9 M) [21] Description: Inhibition of the PD-L1/PD-1 interaction determined in a TR-FRET assay INCB086550 Hs Inhibitor Inhibition >8.0 pIC50 - 23 ⤷ pIC50 >8.0 (IC50 <1x10-8 M) [23] Description: Measuring inhibition of binding of PD-L1 to its receptor PD-1; binned value from patent X14 Hs Inhibitor Binding 7.8 pIC50 - 24 ⤷ pIC50 7.8 (IC50 1.573x10-8 M) [24] Description: Potency of inhibiting PD-1/PD-L1 interaction. BMS-202 Hs Inhibitor Inhibition 7.0 – 7.7 pIC50 - 8,24-25 ⤷ pIC50 7.7 (IC50 1.8x10-8 M) [8] pIC50 7.4 (IC50 3.619x10-8 M) [24] Description: Potency of inhibiting PD-1/PD-L1 interaction. pIC50 7.0 (IC50 9.46x10-8 M) [25] Description: Inhibition of the PD-L1/PD-1 interaction determined by an HTRF FRET-based assay. PD-L1/VISTA dual inhibitor P17 Hs Inhibitor Inhibition 6.8 pIC50 - 20 ⤷ pIC50 6.8 (IC50 1.49x10-7 M) [20] Description: Inhibition of PD-L1/PD-1 interaction determined by TR-FRET EP26 Hs Inhibitor Inhibition 5.8 pIC50 - 25 ⤷ pIC50 5.8 (IC50 1.77x10-6 M) [25] Description: Inhibition of PD-L1/PD-1 protein-protein interaction determined in an HTRF FRET-based binding assay. compound T.14 Hs Inhibitor Binding - - - 3 ⤷ [3] Example 4 [WO2017202275A1] Hs None Binding - - - 5 ⤷ [5] bintrafusp alfa Hs Antibody Binding - - - 11 ⤷ [11] sugemalimab Hs Antibody Binding - - - 6 ⤷ [6] adebrelimab Hs Antibody Binding - - - ⤷ benmelstobart Hs Antibody Binding - - - ⤷ tagitanlimab Hs Antibody Binding - - - ⤷ BMS-986238 Hs Inhibitor Inhibition - - - 19 ⤷ [19]

Ligand mentioned in the following text fields
CD molecules comments