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Assay Detail

CHEMBL5731362

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Binding
Surface Plasmon Resonance (SPR) Assay: Binding of inhibitors to expressed cyclophilins was determined using surface plasmon resonance (SPR) experiments. Briefly, avi-tagged cyclophilin proteins with mono-biotinylation were immobilized onto a Biotin CAPture chip (GE Healthcare, cat. #28920234). SPR experiments were carried out on an upgraded Biacore T200 system using a running buffer containing the inhibitor, 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05% P20, and 3% DMSO. Single-cycle kinetics measurements were used to study the interactions between cyclophilin inhibitors and different cyclophlins. Accordingly, compound at various concentrations was injected to the flow cells with a contact time of 1 min each at a flow rate of 50 μL/min. The final dissociation phase lasts for 10 min following the sample injection. Data was analyzed using Biacore T200 Evaluation Software Version 1.0 and a 1:1 binding model was applied to fit the data to obtain kon, koff, and KD.
ChEMBL ↗
321
Total Activities
105
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peptidyl-prolyl cis-trans isomerase B (CHEMBL2075) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic peptides and use as medicines
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 107 9.04 9.52
kon 107 - -
k_off 107 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5812164 — — 3 9.52
CHEMBL5994784 — — 3 9.40
CHEMBL5741417 — — 3 9.40
CHEMBL6048373 — — 3 9.40
CHEMBL6059588 — — 3 9.40
CHEMBL5842043 — — 3 9.40
CHEMBL5759368 — — 3 9.40
CHEMBL6051666 — — 3 9.40
CHEMBL5810211 — — 3 9.40
CHEMBL6062788 — — 3 9.40
CHEMBL5856868 — — 3 9.30
CHEMBL5757514 — — 3 9.30
CHEMBL6058387 — — 3 9.30
CHEMBL6010886 — — 3 9.30
CHEMBL6003202 — — 3 9.30
CHEMBL3344493 — — 3 9.30
CHEMBL3344501 — — 3 9.30
CHEMBL5942857 — — 3 9.30
CHEMBL5798116 — — 3 9.30
CHEMBL5992700 — — 3 9.30
CHEMBL5792144 — — 3 9.30
CHEMBL5791301 — — 3 9.30
CHEMBL6056488 — — 3 9.30
CHEMBL5831563 — — 3 9.30
CHEMBL5988852 — — 3 9.22
CHEMBL6061966 — — 3 9.22
CHEMBL6050788 — — 3 9.22
CHEMBL5877920 — — 3 9.22
CHEMBL6038296 — — 3 9.22
CHEMBL5976250 — — 3 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5812164 — Kd = 0.3 nM 9.52
CHEMBL5810211 — Kd = 0.4 nM 9.40
CHEMBL5759368 — Kd = 0.4 nM 9.40
CHEMBL5741417 — Kd = 0.4 nM 9.40
CHEMBL5842043 — Kd = 0.4 nM 9.40
CHEMBL5994784 — Kd = 0.4 nM 9.40
CHEMBL6062788 — Kd = 0.4 nM 9.40
CHEMBL6048373 — Kd = 0.4 nM 9.40
CHEMBL6059588 — Kd = 0.4 nM 9.40
CHEMBL6051666 — Kd = 0.4 nM 9.40
CHEMBL6003202 — Kd = 0.5 nM 9.30
CHEMBL6056488 — Kd = 0.5 nM 9.30
CHEMBL5856868 — Kd = 0.5 nM 9.30
CHEMBL6058387 — Kd = 0.5 nM 9.30
CHEMBL5831563 — Kd = 0.5 nM 9.30
CHEMBL5791301 — Kd = 0.5 nM 9.30
CHEMBL6010886 — Kd = 0.5 nM 9.30
CHEMBL5792144 — Kd = 0.5 nM 9.30
CHEMBL5992700 — Kd = 0.5 nM 9.30
CHEMBL3344493 — Kd = 0.5 nM 9.30
CHEMBL3344501 — Kd = 0.5 nM 9.30
CHEMBL5757514 — Kd = 0.5 nM 9.30
CHEMBL5942857 — Kd = 0.5 nM 9.30
CHEMBL5798116 — Kd = 0.5 nM 9.30
CHEMBL6038296 — Kd = 0.6 nM 9.22
CHEMBL6061966 — Kd = 0.6 nM 9.22
CHEMBL6023421 — Kd = 0.6 nM 9.22
CHEMBL5867542 — Kd = 0.6 nM 9.22
CHEMBL6050788 — Kd = 0.6 nM 9.22
CHEMBL5976250 — Kd = 0.6 nM 9.22
CHEMBL5877920 — Kd = 0.6 nM 9.22
CHEMBL5988852 — Kd = 0.6 nM 9.22
CHEMBL6044098 — Kd = 0.6 nM 9.22
CHEMBL5821248 — Kd = 0.7 nM 9.15
CHEMBL5902225 — Kd = 0.7 nM 9.15
CHEMBL5960352 — Kd = 0.7 nM 9.15
CHEMBL5967576 — Kd = 0.7 nM 9.15
CHEMBL5983054 — Kd = 0.7 nM 9.15
CHEMBL5757253 — Kd = 0.7 nM 9.15
CHEMBL5859080 — Kd = 0.7 nM 9.15
CHEMBL5974662 — Kd = 0.7 nM 9.15
CHEMBL5812196 — Kd = 0.7 nM 9.15
CHEMBL6062808 — Kd = 0.7 nM 9.15
CHEMBL6062808 — Kd = 0.7 nM 9.15
CHEMBL5922149 — Kd = 0.7 nM 9.15
CHEMBL6026994 — Kd = 0.7 nM 9.15
CHEMBL5962188 — Kd = 0.7 nM 9.15
CHEMBL6018548 — Kd = 0.7 nM 9.15
CHEMBL6046692 — Kd = 0.7 nM 9.15
CHEMBL5866658 — Kd = 0.7 nM 9.15