hIMB1636-MMAE   Click here for help

GtoPdb Ligand ID: 12978

Compound class: Antibody
Comment: hIMB1636-MMAE is an anti-TROP2 antibody-drug conjugate [1]. It binds to TROP2 on cancer cells and induces their death by apoptosis, ADCC and bystander effects. The MMAE (monomethyl auristatin E; a.k.a. vedotin) conjugate is a widely used microtubule disrupting agent that is liberated once the ADC is internalised by target cells. The PubChem ID for MMAE is CID 11542188.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
hIMB1636-MMAE induces G2/M cell cycle arrest and apoptosis of cancer cells in vitro [1]. It kills pancreatic tumour cells with TROP2 overexpression at nanomolar/subnanomolar levels in vitro, and exhibits potent anti-tumour activity in a pancreatic cancer xenograft model.
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
tumor associated calcium signal transducer 2 Hs Antibody Binding 9.1 pKd - 1
⤷ pKd 9.1 (Kd 7x10-10 M) [1]
Description: Binding affinity for recombinant antigen