A series of (R)- 3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives (2) have been prepared using parallel synthesis, and their structure-activity relationship studied. High affinity human 5-HT1B/1D (h5-HT1B/1D) ligands have been identified. (C) 2003 Elsevier Ltd. All rights reserved.