At a glance
What is it—and why does it matter?
In an inositol triphosphate turnover functional assay using [2-3H]myo-inositol in COS 7 cells expressing human ghrelin receptor, CHEMBL500468 shows agonist potency with EC50 = 1.4 nM.
Sources for this introduction: [1]
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
Using an inositol triphosphate turnover assay with [2-3H]myo-inositol in COS 7 cells expressing human ghrelin receptor, CHEMBL500468 achieves a maximal effect (Emax) of 162.0% relative to untreated control under the assay conditions.
- Reported result
- Emax = 162.0 %
- 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
- supports · Source-backed record
“Standard result: Emax = 162.0 %”
ChEMBL activities for CHEMBL500468 · Activity 12098317
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
Mechanism
In a competitive radioligand binding assay using [35S]-MK-0677, CHEMBL500468 inhibits ligand binding to human GHSR1 with an IC50 of 0.25 nM, indicating high-affinity receptor binding under the reported assay conditions.
- Reported result
- IC50 = 0.25 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
- supports · Source-backed record
“Standard result: IC50 = 0.25 nM”
ChEMBL activities for CHEMBL500468 · Activity 439602
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
Mechanism
A FLIPR-based cell assay in H4 cells expressing the human GHS receptor reports agonist potency for CHEMBL500468 with EC50 = 1.4 nM, reflecting concentration for half-maximal functional response in that readout.
- Reported result
- EC50 = 1.4 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
- supports · Source-backed record
“Standard result: EC50 = 1.4 nM”
ChEMBL activities for CHEMBL500468 · Activity 2163153
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
Mechanism
In an inositol triphosphate turnover functional assay using [2-3H]myo-inositol in COS 7 cells expressing human ghrelin receptor, CHEMBL500468 shows agonist potency with EC50 = 1.4 nM.
- Reported result
- EC50 = 1.4 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
- supports · Source-backed record
“Standard result: EC50 = 1.4 nM”
ChEMBL activities for CHEMBL500468 · Activity 12098320
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
Mechanism
In a competitive receptor binding assay (scintillation counting based) using [125I]-His-ghrelin in COS7 cells expressing human ghrelin receptor, CHEMBL500468 shows binding affinity quantified as Ki = 0.7 nM after 75 mins incubation.
- Reported result
- Ki = 0.7 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
- supports · Source-backed record
“Standard result: Ki = 0.7 nM”
ChEMBL activities for CHEMBL500468 · Activity 12098275
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
Mechanism
In a cell-based radioligand binding assay using [125I][His9]-ghrelin, CHEMBL500468 inhibits radioligand binding to cloned human GHSR type I in LLC PK-1 cells with IC50 = 0.39 nM.
- Reported result
- IC50 = 0.39 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
- supports · Source-backed record
“Standard result: IC50 = 0.39 nM”
ChEMBL activities for CHEMBL500468 · Activity 1142729
chembl-activities:chembl500468:993e87b75c11:993e87b75c11
What has been studied?
What the evidence says.
This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.
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, effect, identity, interaction, regulatory, safety
- 35 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (30), assurance_score_below_0.72 (4), current_regulatory_source_required (4), extraction_ambiguity (21), high_risk_requires_regulatory_or_two_independent_sources (4), no_direct_support (33)
These are the limits of this profile, not an exhaustive list of scientific uncertainties.
References + discovery
Open the records yourself.
- ChEMBL activities for CHEMBL500468 ↗
chembl-activities · published 2026-08-26 · retrieved 2026-08-26T20:13:52Z
Publication history and provenance
Version 4 · Automated assessment · 2026-08-26T20:13:52Z
92921d9978442833316d092fe5528cb426e009d743834349c96e9205c6095f30