pe
pep-10299 v1 CC-BY-SA-4.0

Vasopressin-receptor research peptide (CHEMBL1817752)

A small experimental peptide that switches on vasopressin and oxytocin receptors; used only as a lab research tool, never tested in people.

statusbioassayed targetAVPR1A length8 aa refs1
status 5 / 5
prediction metrics boltz-2 2.2.1
ipTM0.983
pTM0.913
avg pLDDT83.7
ranking score0.867
STRUCTURE · PEP-10299 × AVPR1A
ranking0.867
target interface 4.5Å peptide drag rotate · ctrl+scroll zoom · right-click pan
boltz-2 2.2.1 · mmCIF ↓ download
sequence8 aa
158
CFINNCPG
in the news 2 articles
overview readme

What this is

CHEMBL1817752 is an experimental 8-residue peptide (sequence CFINNCPG) developed as part of a medicinal-chemistry effort to build short-acting peptidic agonists at vasopressin-family receptors (Wiśniewski 2011). It is a research compound — characterized in a published bioassay, catalogued in ChEMBL, but never a clinical drug. The two cysteines in its sequence mirror the cyclic scaffold used by native vasopressin and oxytocin, where a disulfide bridge between the two cysteines defines the binding ring.

On this platform the card lists the V1a receptor (AVPR1A) as the primary target, with V1b (AVPR1B) and the oxytocin receptor (OXTR) as secondary annotations. The reported potency in the card's structured metadata is EC50 = 3700 nM (ChEMBL CHEMBL1817752) — a modest, micromolar-range activity characteristic of an early SAR series rather than an optimised lead.

What it does

In the assay context reported by Wiśniewski and colleagues (2011), this scaffold acts as a peptidic agonist at the V1a vasopressin receptor — meaning, when it engages V1a, it triggers the same downstream signalling that native vasopressin does at that receptor (vascular smooth muscle contraction in physiological tissue). The "short-acting" framing in the paper title is the key design intent: the series was built to retain V1a agonist activity while degrading quickly in plasma, giving a more controllable pharmacological profile than the long-lived native hormone.

This particular 8-mer is one member of that exploratory series. With a reported EC50 in the low-micromolar range it is far weaker than native vasopressin, and there is no published evidence that CHEMBL1817752 itself was advanced beyond bench characterization.

Evidence

  • Human: No human data. This is a research compound; no clinical or human-tissue studies are published for CHEMBL1817752 specifically.
  • Animal: No in-vivo data identified in the dossier for this specific analog.
  • In vitro: Receptor-binding / functional characterization in the Wiśniewski (2011) SAR series, with EC50 = 3700 nM recorded in ChEMBL under accession CHEMBL1817752.

Related peptides

This card sits inside the vasopressin scaffold family — small cyclic peptides built on a two-cysteine ring, varying in side-chain identity to tune receptor selectivity and pharmacokinetics:

  • Vasopressin (/card/pep-04423) — the endogenous nonapeptide and reference compound for V1a, V1b, and V2 activity.
  • Desmopressin (/card/pep-10872) — the V2-selective vasopressin analog used clinically for diabetes insipidus and bedwetting.
  • Oxytocin (/card/pep-04424) — the sister nonapeptide, differing from vasopressin at two positions, with its own dedicated receptor.
details expand to inspect
full evidence table1 metrics
metricvaluetool
EC50 3700 nM GPCRDB/ChEMBL
3-letter notation
Cys-Phe-Ile-Asn-Asn-Cys-Pro-Gly
recipeboltz-2 2.2.1
parametervalue
modelboltz-2 2.2.1
weights
hardwarevast_v100_32gb
mlx version
python
random seed1
msa strategycolabfold_local
runtime
predicted by
predicted at2026-05-22
citationbibtex
peptidemodel (2026). Vasopressin-receptor research peptide (CHEMBL1817752) (pep-10299, v1). PeptideModel. https://peptidemodel.com/card/pep-10299
@peptide{pep10299,
  sequence = {CFINNCPG},
  target   = {avpr1a},
  author   = {peptidemodel},
  year     = {2026},
  status   = {bioassayed}
}
related peptides 2 by signal overlap
clinical trials 0 trials · checked 2026-05-22
0
no registered clinical trials as of 2026-05-22; we'll re-check periodically
references 1 papers
[1]
New, Potent, Selective, and Short-Acting Peptidic V1aReceptor Agonists
Wiśniewski, K. et al. Journal of Medicinal Chemistry 2011
supporting
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