cyclosporin A

Ligand id: 1024

Name: cyclosporin A

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Structure and Physico-chemical Properties

2D Structure

View interactive charts of activity data from ChEMBL and GtoPdb across species (New!)

Selectivity at human GPCRs
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Target Type Action Affinity Units Concentration range (M) Reference
FPR1 Antagonist Antagonist 6.2 – 6.3 pEC50 - 9
pEC50 6.2 – 6.3 [9]
Selectivity at human enzymes
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Target Type Action Affinity Units Concentration range (M) Reference
peptidylprolyl isomerase A Inhibitor Inhibition 8.3 pIC50 - 3
pIC50 8.3 (IC50 5x10-9 M) Inhibition of the phosphatase activity of calcineurin in Jurkat cells. [3]
Selectivity at human transporters
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Target Type Action Affinity Units Concentration range (M) Reference
OATP1B1 Inhibitor Inhibition 7.3 pKi - 2,4
pKi 7.3 (Ki 5.1x10-8 M) [2,4]
ABCG2 Inhibitor Inhibition 6.3 pKi - 7
pKi 6.3 (Ki 5x10-7 M) [7]
Description: Inhibition of ABCG2-ATPase activity induced by substrate binding.
Sodium/bile acid and sulphated solute cotransporter 1 Inhibitor Inhibition 5.1 pKi - 1
pKi 5.1 (Ki 7.6x10-6 M) [1]
OATP1B3 Inhibitor Inhibition 6.1 pIC50 - 4,8
pIC50 6.1 (IC50 8x10-7 M) [4,8]
Sodium/bile acid and sulphated solute cotransporter 1 Inhibitor Inhibition 6.0 pIC50 - 5
pIC50 6.0 (IC50 1x10-6 M) [5]