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antibacterial .ai

Data reference

ChEMBL for antibacterial data: what it holds, and what it will not tell you

ChEMBL is the backbone of public bioactivity data. It is also a database, not an opinion, and antibacterial questions are asked per strain.

At a glance

What it is
A curated bioactivity database from EMBL-EBI
Holds
Measured activities extracted from the literature
Antibacterial records
MIC values against named organisms
Does not hold
A ranking, an opinion or a prediction

ChEMBL is a manually curated database of bioactive molecules and their measured activities, maintained by EMBL-EBI. It is the backbone of public bioactivity data, it is free, and for antibacterial work it will answer a lot of questions and refuse to answer the one you actually asked.

What it holds

  • Compounds with structures, identifiers and calculated properties.
  • Assays extracted from the primary literature and from deposited datasets, each tied to a document.
  • Activities: the measured value, its type, its units and its relation, for example an IC50 in nM or a MIC in µg/mL with a greater than relation.
  • Targets, which for antibacterial work are frequently a whole organism rather than a protein.

For antibacterials the important part is that whole organism assays are first class citizens. A MIC against Staphylococcus aureus is stored as an activity against an organism target, not against a purified enzyme, which is exactly the phenotype level data a screening question needs.

The querying pitfalls

Anyone who has assembled a MIC picture from ChEMBL has hit most of these:

PitfallWhat goes wrong
UnitsMIC appears in µg/mL, mg/L, µM and nM. Converting needs the molecular weight and care with salts.
RelationsA value of 64 with a greater than relation is not the same as a value of 64, and averaging them silently is wrong.
Strain granularityTarget records may be a species, a specific strain, or a resistant clinical isolate. These are not interchangeable.
Method variationBroth microdilution, agar dilution and gradient strips give related but not identical numbers.
Assay conditionsMedia, inoculum and serum content change the result, and are often only in the paper, not the record.
DuplicationThe same measurement can appear through several documents.
Sparse coverageMost published compounds have been tested against a handful of organisms, not a panel.

None of this is a criticism of ChEMBL. It is a faithful record of a heterogeneous literature, and a faithful record of a messy field is messy. The conventions behind those numbers are explained under minimum inhibitory concentration.

What it will not tell you

  1. What your compound will do. If it is not in the database, the database is silent. Similarity searching gives you neighbours, not an answer.
  2. Which compound to test next. There is no ranking, because ranking is an opinion and a database does not have opinions.
  3. Why something failed. A high MIC is recorded. Whether it was efflux, porin loss or target mutation is in the discussion section of a paper, if anywhere.
  4. A strain level roll-up. Assembling one means reconciling assays, units and strain designations by hand.

The other public sources worth knowing

  • CO-ADD, the Community for Open Antimicrobial Drug Discovery, which screens submitted compounds against a standard panel and publishes the data.
  • SPARK and other open antibacterial data initiatives aimed specifically at the Gram-negative accumulation problem.
  • PubChem, broader and less curated, useful for coverage.
  • Surveillance reports, which carry MIC50 and MIC90 distributions for circulating isolates rather than for individual compounds. See antimicrobial resistance.

What a screening layer adds on top

Three things, all of which are work you would otherwise do by hand:

  • Roll-up per strain rather than per assay record, with the units and relations reconciled.
  • A mechanism hypothesis for each organism, drawn from the resistance literature rather than from the activity table.
  • A ranking with confidence, so a series becomes a plate list and the rows with no published basis say so instead of being quietly omitted.

The honest caveat: if you screen one compound a month, the manual ChEMBL query is free and perfectly adequate. The case for a screening layer starts when a series arrives and the same afternoon of work has to happen four hundred times.

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Strain panel

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Sample output Ciprofloxacin Fluoroquinolone
Worked example, replaced when you run
Strain MIC (µg/mL) Call Resistance risk Conf.
S. aureus (MRSA) 0.5->32 R Resistant target mutation, grlA and gyrA Fluoroquinolone resistance is widespread in methicillin resistant lineages.
E. coli <=0.015-0.06 S Susceptible efflux, AcrAB-TolC in resistant isolates Potent against wild type; qnr carriage and gyrA changes shift the band sharply.
K. pneumoniae (CRE) 0.5->64 R Resistant gyrA mutation with plasmid qnr Carbapenemase producing isolates almost always carry quinolone resistance too.
A. baumannii 8->64 R Resistant efflux, AdeABC Constitutive efflux plus target changes leave little room at achievable exposure.
P. aeruginosa 0.25-2 I Intermediate efflux, MexAB-OprM Borderline: active on many isolates, lost quickly once efflux is derepressed.
E. faecium (VRE) 4->32 R Resistant target mutation, parC Enterococci are intrinsically poor fluoroquinolone targets.

Why

Ciprofloxacin is a well characterised fluoroquinolone, so the Gram-negative bands are strongly supported by published activity data. The deciding factor across this panel is not target affinity but exposure: efflux in P. aeruginosa and A. baumannii, and acquired target mutation everywhere resistance is already common. Against a modern ESKAPE panel it reads as a Gram-negative agent with two reliable losses.

Closest published analogs

  • Levofloxacin Broadly similar Gram-negative bands, better Gram-positive coverage
  • Delafloxacin Retains activity against many ciprofloxacin resistant staphylococci
Strain MIC (µg/mL) Call Resistance risk Conf.

Why

Closest published analogs

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Computational prediction from published literature. Research use only, not a lab measurement and not clinical guidance.

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