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cyclic peptide HDAC inhibitor

Romidepsin

Published evidence · coverage incomplete

Anatomy in the research

Anatomy evidence is still being assembled.

These are anatomical mentions in cited research—not established treatment targets or proof of benefit in people.

This publication has no anatomy passages that meet our source-linking checks yet. Read the available findings ↓

General anatomy view only. No peptide-specific structures are highlighted.

At a glance

What is it—and why does it matter?

An introduction is not yet available. The findings below address specific research questions, not a complete account of this peptide.

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

How does it work?

Target, response, and disposition.

Mechanism

In a single-protein biochemical assay, romidepsin inhibits human histone deacetylase 3 (HDAC3) with Ki = 0.15 nM, reflecting high potency.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: Histone deacetylase 3 (CHEMBL1829) Assay: Inhibition of human HDAC3 Assay format: single protein format Standard result: Ki = 0.15 nM pChEMBL value: 9.82 Document: CHEMBL1212811
Reported result
Ki = 0.15 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: Histone deacetylase 3 (CHEMBL1829) Assay: Inhibition of human HDAC3 Assay format: single protein format Standard result: Ki = 0.15 nM pChEMBL value: 9.82 Document: CHEMBL1212811”

    ChEMBL activities for CHEMBL343448 · Activity 3389935

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Mechanism

In a purified single-protein assay, romidepsin inhibits human histone deacetylase 2 (HDAC2) with a Ki of 0.038 nM, indicating very high potency.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: Histone deacetylase 2 (CHEMBL1937) Assay: Inhibition of human HDAC2 Assay format: single protein format Standard result: Ki = 0.038 nM pChEMBL value: 10.42 Document: CHEMBL1212811
Reported result
Ki = 0.038 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: Histone deacetylase 2 (CHEMBL1937) Assay: Inhibition of human HDAC2 Assay format: single protein format Standard result: Ki = 0.038 nM pChEMBL value: 10.42 Document: CHEMBL1212811”

    ChEMBL activities for CHEMBL343448 · Activity 3389934

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Mechanism

In a purified single-protein assay, romidepsin shows very high binding potency toward human histone deacetylase 1 (HDAC1), quantified as a Ki of 0.0015 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: Histone deacetylase 1 (CHEMBL325) Assay: Inhibition of human HDAC1 Assay format: single protein format Standard result: Ki = 0.0015 nM Document: CHEMBL1212811
Reported result
Ki = 0.0015 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: Histone deacetylase 1 (CHEMBL325) Assay: Inhibition of human HDAC1 Assay format: single protein format Standard result: Ki = 0.0015 nM Document: CHEMBL1212811”

    ChEMBL activities for CHEMBL343448 · Activity 3389933

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Mechanism

In a purified single-protein assay, romidepsin inhibits human protein deacetylase HDAC6 with Ki = 9.5 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: Protein deacetylase HDAC6 (CHEMBL1865) Assay: Inhibition of human HDAC6 Assay format: single protein format Standard result: Ki = 9.5 nM pChEMBL value: 8.02 Document: CHEMBL1212811
Reported result
Ki = 9.5 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: Protein deacetylase HDAC6 (CHEMBL1865) Assay: Inhibition of human HDAC6 Assay format: single protein format Standard result: Ki = 9.5 nM pChEMBL value: 8.02 Document: CHEMBL1212811”

    ChEMBL activities for CHEMBL343448 · Activity 3389938

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Pharmacokinetics

Reported human pharmacokinetics after intravenous administration include a mean residence time (MRT) of 2.6 hr.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Mean residence time in human after iv administration Assay format: organism-based format Standard result: MRT = 2.6 hr Document: CHEMBL1614632
Reported result
MRT = 2.6 hr
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Mean residence time in human after iv administration Assay format: organism-based format Standard result: MRT = 2.6 hr Document: CHEMBL1614632”

    ChEMBL activities for CHEMBL343448 · Activity 5081806

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Pharmacokinetics

Reported human pharmacokinetics after intravenous administration include a steady-state volume of distribution (Vdss) of 1.2 L.kg-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Volume of distribution at steady state in human after iv administration Assay format: organism-based format Standard result: Vdss = 1.2 L.kg-1 Document: CHEMBL1614632
Reported result
Vdss = 1.2 L.kg-1
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Volume of distribution at steady state in human after iv administration Assay format: organism-based format Standard result: Vdss = 1.2 L.kg-1 Document: CHEMBL1614632”

    ChEMBL activities for CHEMBL343448 · Activity 5081096

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Pharmacokinetics

Reported human pharmacokinetics after intravenous administration include an elimination half-life (T1/2) of 11.0 hr.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Half life in human after iv administration Assay format: organism-based format Standard result: T1/2 = 11.0 hr Document: CHEMBL1614632
Reported result
T1/2 = 11.0 hr
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Half life in human after iv administration Assay format: organism-based format Standard result: T1/2 = 11.0 hr Document: CHEMBL1614632”

    ChEMBL activities for CHEMBL343448 · Activity 5082985

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Pharmacokinetics

Reported human pharmacokinetics after intravenous administration include systemic clearance (CL) of 7.4 mL.min-1.kg-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Clearance in human after iv administration Assay format: organism-based format Standard result: CL = 7.4 mL.min-1.kg-1 Document: CHEMBL1614632
Reported result
CL = 7.4 mL.min-1.kg-1
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: ADMET (CHEMBL612558) Assay: Clearance in human after iv administration Assay format: organism-based format Standard result: CL = 7.4 mL.min-1.kg-1 Document: CHEMBL1614632”

    ChEMBL activities for CHEMBL343448 · Activity 5082656

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

What has been studied?

What the evidence says.

Study findings

An organism-based assay in human naive CD4+ T cells reports that romidepsin reactivates latent HIV1 NL4-3-Luc expression with EC50 = 3.0 nM when measured after 48 hrs.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: Human immunodeficiency virus 1 (CHEMBL378) Assay: Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis Assay format: organism-based format Standard result: EC50 = 3.0 nM pChEMBL value: 8.52 Document: CHEMBL3124835
Reported result
EC50 = 3.0 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: Human immunodeficiency virus 1 (CHEMBL378) Assay: Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis Assay format: organism-based format Standard result: EC50 = 3.0 nM pChEMBL value: 8.52 Document: CHEMBL3124835”

    ChEMBL activities for CHEMBL343448 · Activity 13944699

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Study findings

In a cell-based growth inhibition assay, romidepsin shows sub-nanomolar potency against the MCF7 cell line, with IC50 = 0.75 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL343448Molecule: CHEMBL343448 Target: MCF7 (CHEMBL387) Assay: Growth inhibition of MCF7 cells Assay format: cell-based format Standard result: IC50 = 0.75 nM pChEMBL value: 9.12 Document: CHEMBL1138260
Reported result
IC50 = 0.75 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL343448 Target: MCF7 (CHEMBL387) Assay: Growth inhibition of MCF7 cells Assay format: cell-based format Standard result: IC50 = 0.75 nM pChEMBL value: 9.12 Document: CHEMBL1138260”

    ChEMBL activities for CHEMBL343448 · Activity 2000978

    chembl-activities:chembl343448:53231463e4d2:53231463e4d2

Risks and interactions

Risks, organized for scanning.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Products and regulatory status

Same ingredient. Different records.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, contraindication, identity, interaction, regulatory, safety
  • 64 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (41), assurance_score_below_0.72 (21), current_regulatory_source_required (12), extraction_ambiguity (59), high_risk_requires_regulatory_or_two_independent_sources (21), no_direct_support (61)
  • A source-backed introductory overview is not yet available.

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL343448 ↗

    chembl-activities · published 2026-08-29 · retrieved 2026-08-29T08:37:13Z

Publication history and provenance

Version 1 · Automated assessment · 2026-08-29T08:37:13Z

a2f4d31d49e960235a3cef19f949be1b8da5adc4ce1ef8099aae7826821f5287